1,734 results match your criteria Bioorganic chemistry[Journal]


Discovery of cycloneolignan enantiomers from Isatis indigotica Fortune with neuroprotective effects against MPP-induced SH-SY5Y cell injury.

Bioorg Chem 2019 Apr 15;88:102926. Epub 2019 Apr 15.

School of Traditional Chinese Materia Medica, Key Laboratory of Computational Chemistry-Based Natural Antitumor Drug Research & Development, Liaoning Province, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China. Electronic address:

A pair of new cycloneolignan enantiomers (1a and 1b) were isolated from the leaves of Isatis indigotica Fortune. Their structures were elucidated by extensive spectroscopic data analysis, including 1D and 2D NMR, HRESIMS, MS/MS analysis, together with theoretical electronic circular dichroism (ECD) calculations. Compounds 1a and 1b were then evaluated for their neuroprotective effects against MPP-induced SH-SY5Y cell injury. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.102926DOI Listing

Cisplatin: The first metal based anticancer drug.

Authors:
Sumit Ghosh

Bioorg Chem 2019 Apr 11;88:102925. Epub 2019 Apr 11.

Department of Chemistry, Indian Institute of Technology Kanpur, Kanpur, Uttar Pradesh 208016, India. Electronic address:

Cisplatin or (SP-4-2)-diamminedichloridoplatinum(II) is one of the most potential and widely used drugs for the treatment of various solid cancers such as testicular, ovarian, head and neck, bladder, lung, cervical cancer, melanoma, lymphomas and several others. Cisplatin exerts anticancer activity via multiple mechanisms but its most acceptable mechanism involves generation of DNA lesions by interacting with purine bases on DNA followed by activation of several signal transduction pathways which finally lead to apoptosis. However, side effects and drug resistance are the two inherent challenges of cisplatin which limit its application and effectiveness. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.102925DOI Listing
April 2019
1 Read

6-Methoxyflavonols from the aerial parts of Tetragonia tetragonoides (Pall.) Kuntze and their anti-inflammatory activity.

Bioorg Chem 2019 Apr 11;88:102922. Epub 2019 Apr 11.

Graduate School of Biotechnology and Department of Oriental Medicinal Biotechnology, Kyung Hee University, Yongin 17104, Republic of Korea. Electronic address:

Dried aerial parts of Tetragonia tetragonoides were extracted with 70% EtOH, and the evaporated residue was successively separated into EtOAc, n-BuOH, and HO fractions. As a result of repeated SiO, ODS, and Sephadex LH-20 column chromatography, four new 6-methoxyflavonol glycosides (2-4, 8) along with four known ones (1, 5-7) were isolated. Several spectroscopic data led to determination of chemical structures for four new 6-methoxyflavonol glycosides (2-4, 8) and four known ones, 6-methoxykaempferol 3-O-β-d-glucopyranosyl-(1 → 2)-β-d-glucopyranosyl-7-O-(6‴'-(E)-caffeoyl)-β-d-glucopyranoside (1), 6-methoxyquercetin (5), 6-methoxykaempferol (6), and 6-methoxykaempferol 7-O-β-d-glucopyranoside (7). Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.102922DOI Listing

Synthesis, biological activity and multiscale molecular modeling studies of bis-coumarins as selective carbonic anhydrase IX and XII inhibitors with effective cytotoxicity against hepatocellular carcinoma.

Bioorg Chem 2019 Mar 7;87:838-850. Epub 2019 Mar 7.

Sakarya University of Applied Sciences, Pamukova Vocational Highschool, Pamukova, Turkey.

A series of novel bis-coumarin derivatives containing triazole moiety as a linker between the alkyl chains was synthesized and their inhibitory activity against the human carbonic anhydrase (hCA) isoforms I, II, IX and XII were evaluated. In addition, cytotoxic effects of the synthesized compounds on renal adenocarcinoma (769P), hepatocellular carcinoma (HepG2) and breast adeno carcinoma (MDA-MB-231) cell lines were examined. While the hCA I and II isoforms were inhibited in the micromolar range, the tumor-associated isoform hCA IX and XII were inhibited in the high nanomolar range. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.003DOI Listing

Hydrazones as novel epigenetic modulators: Correlation between TET 1 protein inhibition activity and their iron(II) binding ability.

Bioorg Chem 2019 Feb 16;88:102809. Epub 2019 Feb 16.

BIOCEV, First Faculty of Medicine, Charles University, Průmyslová 595, 252 50 Vestec, Czech Republic; Department of Analytical Chemistry, Faculty of Chemical Engineering, University of Chemistry and Technology, Technická 5, 166 28 Prague 6, Czech Republic; Department of Paediatrics and Adolescent Medicine, First Faculty of Medicine, Charles University, Ke Karlovu 2, 121 08 Prague 2, Czech Republic. Electronic address:

Ten-eleven translocation protein (TET) 1 plays a key role in control of DNA demethylation and thereby of gene expression. Dysregulation of these processes leads to serious pathological states such as oncological and neurodegenerative ones and thus TET 1 targeting is highly requested. Therefore, in this work, we examined the ability of hydrazones (acyl-, aroyl- and heterocyclic hydrazones) to inhibit the TET 1 protein and its mechanism of action. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.02.034DOI Listing
February 2019

Potent and selective EGFR inhibitors based on 5-aryl-7H-pyrrolopyrimidin-4-amines.

Bioorg Chem 2019 Apr 11;88:102918. Epub 2019 Apr 11.

Department of Chemistry, Norwegian University of Science and Technology (NTNU), NO-7491 Trondheim, Norway. Electronic address:

The epidermal growth factor receptor represents an important target in cancer therapy, and low molecular weight inhibitors based on quinazolines have reached the marked. Herein we report on a new scaffold, 5-aryl-7H-pyrrolo[2,3-d]pyrimidin-4-amines, and show that when employing (S)-phenylglycinol as C-4 substituent, potent inhibitors can be made. The two most active inhibitors have suitable druglike properties, were equipotent with Erlotinib in Ba/F3 cell studies, and showed lower cross reactivity than Erlotinib in a panel of 50 kinases. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00452068193000
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http://dx.doi.org/10.1016/j.bioorg.2019.102918DOI Listing
April 2019
1 Read

Vieloplains A-G, seven new guaiane-type sesquiterpenoid dimers from Xylopia vielana.

Bioorg Chem 2019 Apr 10;88:102891. Epub 2019 Apr 10.

Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, PR China; Institute of Interdisciplinary Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, PR China; School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China. Electronic address:

Seven new guaiane-type sesquiterpene dimers vieloplains A-G, connecting patterns through three different direct CC bonds compounds 1-5 (C-3 to C-3', C-4 to C-1'), compound 6 (C-2 to C-3', C-4 to C-2') and compound 7 (C-2 to C-1', C-4 to C-2') were isolated from the roots of Xylopia vielana. Their absolute configurations were established by NOESY analysis, the Cu Kα X-ray crystallographic the experiment circular dichroism (ECD) and the calculated ECD. Among them, only compound 6 showed a considerable cytotoxicity against DU145 cells with IC values of 9. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.065DOI Listing

Synthesis and biological evaluation of purine-pyrazole hybrids incorporating thiazole, thiazolidinone or rhodanine moiety as 15-LOX inhibitors endowed with anticancer and antioxidant potential.

Bioorg Chem 2019 Apr 1;87:821-837. Epub 2019 Apr 1.

Genetic Engineering and Biotechnology Research Institute (GEBRI), City for Scientific Research and Technology, Alexandria, Egypt.

Novel purine-pyrazole hybrids combining thiazoles, thiazolidinones and rhodanines, were designed and tested as 15-LOX inhibitors, potential anticancer and antioxidant agents. All tested compounds were found to be potent 15-LOX inhibitors with IC ranging from 1.76 to 6. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.076DOI Listing
April 2019
1 Read

Glucosamine-6-phosphate synthase inhibiting C3-β-cholesterol tethered spiro heterocyclic conjugates: Synthesis and their insight of DFT and docking study.

Bioorg Chem 2019 Apr 9;88:102920. Epub 2019 Apr 9.

Department of Chemistry, College of Science, King Saud University, Riyadh, Saudi Arabia. Electronic address:

A series of novel covalent cholesterol-spiro pyrrolidine/pyrrolizidine heterocyclic hybrids possessing biologically active oxindole, indanedione, and acenaphthylene-1-one have been synthesized by the reaction of C3-β-cholesteroalacrylate with heterocyclic di- and tri-ketones. All the sixteen compounds were obtained as a single isomer in good yield through a stereo- and regio- selective 1,3-dipolar cycloaddition methodology. Stereochemistry of the spiranic cycloadducts has been established by spectroscopic analysis and the regioselectivity outcome of the spiro adducts has been accomplished by DFT calculations at B3LYP/6-31G (d,p) level study. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.102920DOI Listing

Facile one-pot synthesis, antiproliferative evaluation and structure-activity relationships of 3-amino-1H-indoles and 3-amino-1H-7-azaindoles.

Bioorg Chem 2019 Apr 10;88:102914. Epub 2019 Apr 10.

Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Science, Southern Medical University, Guangzhou 510515, PR China. Electronic address:

A highly efficient method has been developed for the one-pot synthesis of substituted 3-amino-1H-indole and 3-amino-1H-7-azaindole derivatives starting from ethyl 2-cyanophenylcarbamate/ethyl 3-cyanopyridin-2-ylcarbamate, and α-bromoketones in good to excellent yields. All newly synthesized analogues were screened for their antiproliferative activities against four cancer cell lines. The most promising compound 8v demonstrated 13-, 5-, and 1. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00452068183134
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http://dx.doi.org/10.1016/j.bioorg.2019.04.008DOI Listing
April 2019
3 Reads

Identification of novel imidazole flavonoids as potent and selective inhibitors of protein tyrosine phosphatase.

Bioorg Chem 2019 Apr 9;88:102900. Epub 2019 Apr 9.

Laboratory of Bioorganic & Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, People's Republic of China.

A series of imidazole flavonoids as new type of protein tyrosine phosphatase inhibitors were synthesized and characterized. Most of them gave potent protein phosphatase 1B (PTP1B) inhibitory activities. Especially, compound 11a could effectively inhibit PTP1B with an IC value of 0. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.074DOI Listing

Chemical constituents from Vietnamese mangrove Calophyllum inophyllum and their anti-inflammatory effects.

Bioorg Chem 2019 Apr 11;88:102921. Epub 2019 Apr 11.

College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea. Electronic address:

In a search for anti-inflammatory activity in resources from Vietnamese mangroves, we found that a methanolic extract from the leaves of Calophyllum inophyllum (CIL) showed significant anti-inflammatory effects in vitro. Using various chromatographic techniques, we subsequently isolated 12 compounds (1-12) from a methanolic extract of CIL, including two novel compounds (1-2). The inhibitory effects of these compounds on lipopolysaccharide-induced nitric oxide (NO) production in RAW264. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00452068193016
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http://dx.doi.org/10.1016/j.bioorg.2019.102921DOI Listing
April 2019
3 Reads

Substituted 1,3-dioxoisoindoline-4-aminoquinolines coupled via amide linkers: Synthesis, antiplasmodial and cytotoxic evaluation.

Bioorg Chem 2019 Apr 11;88:102912. Epub 2019 Apr 11.

Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India. Electronic address:

Synthesis of C-5-substituted 1,3-dioxoisoindoline-4-aminoquinolines having amide group as a spacer was developed with an intent to evaluate their antiplasmodial activities. The synthesized dioxoisoindoline-aminoquinolines tethered with β-alanine as a spacer and secondary amine as substituent displayed good anti-plasmodial activities. Compound 7j, with an optimum combination of β-alanine and an ethyl chain length as linker along with diethylamine as the secondary amine counterpart at dioxoisoindoline proved to be most potent and non-cytotoxic with IC of 0. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.04.006DOI Listing

Synthesis, antitumor testing and molecular modeling study of some new 6-substituted amido, azo or thioureido-quinazolin-4(3H)-ones.

Bioorg Chem 2019 Apr 10;88:102923. Epub 2019 Apr 10.

Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, P.O. Box 35516, Mansoura, Egypt. Electronic address:

A new series of 6-substituted amido, azo or thioureido-quinazolin-4(3H)-one was synthesized and tested for their in-vitro antitumor activity. Compounds 21, 53 and 60 showed broad spectrum antitumor activity with average IC values of 6.7, 7. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00452068193014
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http://dx.doi.org/10.1016/j.bioorg.2019.102923DOI Listing
April 2019
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Probing the high potency of pyrazolyl pyrimidinetriones and thioxopyrimidinediones as selective and efficient non-nucleotide inhibitors of recombinant human ectonucleotidases.

Bioorg Chem 2019 Apr 2;88:102893. Epub 2019 Apr 2.

Centre for Advanced Drug Research, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan. Electronic address:

With the aim to discover novel, efficient and selective inhibitors of human alkaline phosphatase and nucleotide pyrophosphatase enzymes, two new series of pyrazolyl pyrimidinetriones (PPTs) (6a-g) and thioxopyrimidinediones (PTPs) (6h-n) were synthesized in good chemical yields using Knoevenagel condensation reaction between pyrazole carbaldehydes (4a-g) and pharmacologically active N-alkylated pyrimidinetrione (5a) and thioxopyrimidinedione (5b). The inhibition potential of the synthesized hybrid compounds was evaluated against human alkaline phosphatase (h-TNAP and h-IAP) and ectonucleotidase (h-NPP1 and h-NPP3) enzymes. Most of the tested analogs were highly potent with a variable degree of inhibition depending on the functionalized hybrid structure. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00452068183098
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http://dx.doi.org/10.1016/j.bioorg.2019.03.067DOI Listing
April 2019
2 Reads

Evaluation of angularly condensed diquinothiazines as potential anticancer agents.

Bioorg Chem 2019 Apr 6;87:810-820. Epub 2019 Apr 6.

The Medical University of Silesia, School of Pharmacy with the Division of Laboratory Medicine, Department of Cell Biology, Jedności 8, 41-200 Sosnowiec, Poland.

We present efficient synthesis of isomeric types of angularly fused diquinothiazines in the reactions of 2,2'-dichloro-3,3'-diquinolinyl disulfide and diquinodithiin with 3-, 5-, 6- and 8-aminoquinolines. The pentacyclic diquinothiazine ring systems were identified as diquino[3,2-b;3',4'-e][1,4]thiazine, diquino[3,2-b;5',6'-e][1,4]thiazine, diquino[3,2-b;6',5'-e][1,4]thiazine and diquino[3,2-b;8',7'-e][1,4]thiazine with advanced two-dimensional H and C NMR techniques (COSY, ROESY, HSQC and HMBC) of N-methyl derivatives. The identification of pentacyclic ring system was confirmed by X-ray diffraction analysis of selected N-alkyl derivatives. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.04.005DOI Listing

Targeting hepatocellular carcinoma: Synthesis of new pyrazole-based derivatives, biological evaluation, DNA binding, and molecular modeling studies.

Bioorg Chem 2019 Apr 8;88:102917. Epub 2019 Apr 8.

Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.

A new series of pyrazole derivatives was prepared in this work, including pyrazolopyrimidines, pyrazolotriazines, pyrazolylthienopyridines, and 2-(pyrazolylamino)thiazol-4-ones, utilizing 3-amino-5-methyl-1H-pyrazole as a synthetic precursor. Their in vitro anticancer activity was tested on hepatocellular carcinoma cell line, HepG2. The results revealed that the pyrazolylhydrazonoyl cyanide 8, the pyrazolopyrimidine 3, and the pyrazolylaminothiazolone 17 were the most active with IC values of 2, 7, and 7 µM respectively in comparison with 5. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.04.011DOI Listing

Mechanistic investigation of anthocyanidin derivatives as α-glucosidase inhibitors.

Bioorg Chem 2019 Jan 22;87:803-809. Epub 2019 Jan 22.

Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup 56212, Republic of Korea. Electronic address:

Eight anthocyanidin derivatives (1-8) were evaluated as potential inhibitors of the catalysis of α-glucosidase. Among them, compounds 4 and 8 had the highest levels of inhibitory activity at 100 μM (IC values of 14.4 ± 0. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00452068183134
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http://dx.doi.org/10.1016/j.bioorg.2019.01.033DOI Listing
January 2019
1 Read
2.152 Impact Factor

Novel synthesized SLC-0111 thiazole and thiadiazole analogues: Determination of their carbonic anhydrase inhibitory activity and molecular modeling studies.

Bioorg Chem 2019 Apr 3;87:794-802. Epub 2019 Apr 3.

Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Polo Scientifico, Via U. Schiff 6, 50019, Sesto Fiorentino, Firenze, Italy. Electronic address:

In the presented work, we report the design and synthesis of novel SLC-0111 thiazole and thiadiazole analogues (11a-d, 12a-d, 16a-c and 17a-d). A bioisosteric replacement approach was adopted to replace the 4-fluorophenyl tail of SLC-0111 with thiazole and thiadiazole ones, which were thereafter extended with lipophilic un/substituted phenyl moieties. All the newly synthesized SLC-0111 analogues were evaluated in vitro for their inhibitory activity towards a panel of the metalloenzyme carbonic anhydrase (CA, EC 4. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.04.002DOI Listing
April 2019
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Furofuran lignans as a new series of antidiabetic agents exerting α-glucosidase inhibition and radical scarvenging: Semisynthesis, kinetic study and molecular modeling.

Bioorg Chem 2019 Apr 5;87:783-793. Epub 2019 Apr 5.

Center of Excellence in Natural Product, Department of Chemistry, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand. Electronic address:

A new series of furofuran lignans containing catechol moiety were prepared from the reactions between lignans and a variety of phenolics. All 22 products obtained were evaluated against three different α-glucosidases (maltase, sucrase and Baker's yeast glucosidase) and DPPH radical. Of furofuran lignans evaluated, β-14, having two catechol moieties and one acetoxy group, was the most potent inhibitor against Baker's yeast, maltase, and sucrase with IC values of 5. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.077DOI Listing

Probing the antibacterial and anticancer potential of tryptamine based mixed ligand Schiff base Ruthenium(III) complexes.

Bioorg Chem 2019 Apr 4;87:773-782. Epub 2019 Apr 4.

Bioinorganic Lab., Department of Chemistry, Jamia Millia Islamia, New Delhi 110025, India. Electronic address:

Development of new chemotherapeutic agents to treat microbial infections and recurrent cancers is of pivotal importance. Metal based drugs particularly ruthenium complexes have the uniqueness and desired properties that make them suitable candidates for the search of potential chemotherapeutic agents. In this study, two mixed ligand Ru(III) complexes [Ru(Cl)(SB)(Phen] (RC-1) and [Ru(Cl)(SB)(Bipy)] (RC-2) were synthesised and characterized by elemental analysis, IR, UV-Vis, H, C NMR spectroscopic techniques and their molecular structure was confirmed by X-ray crystallography. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.080DOI Listing
April 2019
2 Reads

Synthesis and biological evaluation of coumarin-1,3,4-oxadiazole hybrids as selective carbonic anhydrase IX and XII inhibitors.

Bioorg Chem 2019 Apr 5;87:765-772. Epub 2019 Apr 5.

Università degli Studi di Firenze, Neurofarba Dept., Sezione di Scienze Farmaceutiche e Nutraceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy. Electronic address:

With an aim to develop novel heterocyclic hybrids as potent anticancer agents, we synthesized a series of coumarin-1,3,4-oxadiazole hybrids (7a-t) and evaluated for their inhibitory activity against the four physiologically relevant human carbonic anhydrase (hCA, EC 4.2.1. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.04.004DOI Listing

Design, synthesis and biological evaluation of Helicobacter pylori inosine 5'-monophosphate dehydrogenase (HpIMPDH) inhibitors. Further optimization of selectivity towards HpIMPDH over human IMPDH2.

Bioorg Chem 2019 Apr 4;87:753-764. Epub 2019 Apr 4.

Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM's NMIMS (Deemed to be University), V. L. Mehta Road, Vile Parle (West), Mumbai 400 056, India. Electronic address:

Inosine 5'-monophosphate dehydrogenase (IMPDH, EC 1.1.1. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.04.001DOI Listing

Antioxidant and angiotensin-converting enzyme (ACE) inhibitory activity of thymosin alpha-1 (Thα1) peptide.

Bioorg Chem 2019 Apr 4;87:743-752. Epub 2019 Apr 4.

Research Center for Molecular Medicine, Hamadan University of Medical Sciences, Hamadan, Iran.

In this research, the antioxidant property of thymosin alpha-1 (Thα1) peptide was investigated through various antioxidant methods. Thα1 showed 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity (IC = 20 µM) and its 2,2-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) scavenging reached 45.33% at 80 µM (IC = 85 µM). Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.04.003DOI Listing

Natural flavonoid α-glucosidase inhibitors from Retama raetam: Enzyme inhibition and molecular docking reveal important interactions with the enzyme active site.

Bioorg Chem 2019 Apr 1;87:736-742. Epub 2019 Apr 1.

Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box. 2457, Riyadh 11451, Saudi Arabia.

Retama raetam (Forsk.) Webb & Berthel plant has been traditionally used for the treatment of diabetes mellitus and hypertension. Interest in the medicinal chemistry of the plant in the past resulted in the isolation of a number of compounds with anti-hyperglycemic activity. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.079DOI Listing
April 2019
2 Reads

Lithocarols A-F, six tenellone derivatives from the deep-sea derived fungus Phomopsis lithocarpus FS508.

Bioorg Chem 2019 Apr 1;87:728-735. Epub 2019 Apr 1.

State Key Laboratory of Applied Microbiology Southern China, Guangdong Provincial Key Laboratory of Microbial Culture Collection and Application, Guangdong Open Laboratory of Applied Microbiology, Guangdong Institute of Microbiology, Guangzhou 510070, China. Electronic address:

Lithocarols A-F (1-6) possessing novel highly-oxygenated isobenzofuran core, together with a related known compound isoprenylisobenzofuran A (7) were isolated from the marine-derived fungus Phomopsis lithocarpus FS508. Among them, lithocarols A-E (1-5) represent the first examples of poly-ketal derivatives in tenellone family. The structures for all these compounds were fully elucidated by spectroscopic analysis, X-ray diffraction, and electronic circular dichroism calculations. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.078DOI Listing

Design, synthesis and evaluation of a novel metal chelator as multifunctional agents for the treatment of Alzheimer's disease.

Bioorg Chem 2019 Mar 28;87:720-727. Epub 2019 Mar 28.

School of Chemistry and Chemical Engineering, Southeast University, Nanjing, Jiangsu 211189, PR China; Suzhou Key Laboratory of Biomaterials and Technologies & Collaborative Innovation Center of Suzhou Nano Science and Technology, Suzhou 215123, PR China. Electronic address:

A series of compounds following the lead compounds including deferasirox and tacrine were designed, synthesized and evaluated as multifunctional agents against Alzheimer's disease (AD). In vitro studies showed that most synthesized compounds exhibited good multifunctional activities in inhibiting acetylcholinesterase (bAChE), and chelating metal ions. Especially, compound TD demonstrated significant metal chelating property, a moderate acetylcholinesterase (AChE) inhibitory activity and an antioxidant activity. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.064DOI Listing
March 2019
2 Reads
2.152 Impact Factor

Glycopentanolones A-D, four new geranylated quinolone alkaloids from Glycosmis pentaphylla.

Bioorg Chem 2019 Mar 28;87:714-719. Epub 2019 Mar 28.

Bio-Center, Gyeonggido Business & Science Accelerator (GBSA), Suwon 16229, Republic of Korea. Electronic address:

The ethanolic extract obtained from the stems of Glycosmis pentaphylla was found to suppress antigen-mediated degranulation of rat basophilic leukemia (RBL-2H3) cells. Four new geranylated 2-quinolone alkaloids, named glycopentanolones A-D (1-4), and 12 known metabolites (5-16) were isolated from the ethanolic extract from the stems of G. pentaphylla using bioassay-guided fractionation. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.069DOI Listing
March 2019
1 Read
2.152 Impact Factor

Design and synthesis of parthenolide-SAHA hybrids for intervention of drug-resistant acute myeloid leukemia.

Bioorg Chem 2019 Mar 22;87:699-713. Epub 2019 Mar 22.

State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Haihe Education Park, 38 Tongyan Road, Tianjin 300353, People's Republic of China. Electronic address:

A series of parthenolide-SAHA hybrids were synthesized and evaluated for their anti-AML activities against HL-60 and HL-60/ADR cell lines. The most active compound 26 exhibited high activity against HL-60/ADR cell line with IC value of 0.15 μM, which demonstrated 16. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.056DOI Listing
March 2019
2 Reads

Sanggenon O induced apoptosis of A549 cells is counterbalanced by protective autophagy.

Bioorg Chem 2019 Apr 3;87:688-698. Epub 2019 Apr 3.

Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, PR China; Key Laboratory of Advanced Drug Preparation Technologies (Zhengzhou University), Ministry of Education of China, PR China; Key Laboratory of Henan Province for Drug Quality and Evaluation, PR China; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China. Electronic address:

Sanggenon O (SO) is a Diels-Alder type adduct extracted fromMorus alba, which has been used for its anti-inflammatory action in the Oriental medicine. However, whether it has regulatory effect on human cancer cell proliferation and what the underlying mechanism remains unknown. Here, we found that SO could significantly inhibit the growth and proliferation of A549 cells and induce its pro-apoptotic action through a caspase-dependent pathway. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.072DOI Listing
April 2019
2 Reads

5-Thioxoimidazolidine-2-one derivatives: Synthesis, anti-inflammatory activity, analgesic activity, COX inhibition assay and molecular modelling study.

Bioorg Chem 2019 Apr 1;87:679-687. Epub 2019 Apr 1.

Applied Organic Chemistry Department, National Research Centre, Cairo, Egypt.

A series of 5-imino-4-thioxo-2-imidazolidinone derivatives with different substituents at N and N was synthesized with high yield and excellent purity by the reaction of different N-arylcyanothioformamide derivatives with isocyanate derivatives. Treatment 5-imino-4-thioxo-2-imidazolidinone derivatives with acidic medium afforded 4-thioxoimidazolidin-2,5-dione derivatives. The structures of the obtained products were established based on spectroscopic IR, H NMR, C NMR, H, H-COSY, HSQC and elemental analyses. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00452068183143
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http://dx.doi.org/10.1016/j.bioorg.2019.03.075DOI Listing
April 2019
3 Reads

Unveiling novel diphenyl-1H-pyrazole based acrylates tethered to 1,2,3-triazole as promising apoptosis inducing cytotoxic and anti-inflammatory agents.

Bioorg Chem 2019 Mar 29;87:667-678. Epub 2019 Mar 29.

Drug Design and Medicinal Chemistry Lab, Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, India. Electronic address:

Meagre and suboptimal therapeutic response along with the side effect profile associated with the existing anticancer therapy have necessitated the development of new therapeutic modalities to curb this disease. Bearing in mind the current scenario, a series of 1,2,3-triazole linked 3-(1,3-diphenyl-1H-pyrazol-4-yl)acrylates was synthesized following a multi-step reaction scheme. Initial screening for anticancer potential was done by in vitro sulforhodamine B assay against four human cancer cell lines- MCF-7 (breast), A549 (Lung) and HCT-116 and HT-29 (Colon). Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.071DOI Listing
March 2019
2 Reads

Hydrolysis of surfactin over activated carbon.

Bioorg Chem 2019 Apr 2. Epub 2019 Apr 2.

Biotransformation Department, Faculty of Biotechnology, University of Wrocław, Fryderyka Joliot-Curie Str. 14a, 50-383 Wrocław, Poland; InventionBio, Wojska Polskiego 65, 85-825 Bydgoszcz, Poland. Electronic address:

Surfactin is obtained through biocatalysis by microorganisms. In our biorefinery concept, it is purified on activated carbon (AC) during downstream processing. Besides cyclic surfactin, it is possible to obtain linear surfactin analogues, when AC with specific properties is used. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.070DOI Listing

Design and synthesis of novel PARP-1 inhibitors based on pyridopyridazinone scaffold.

Bioorg Chem 2019 Mar 28;87:655-666. Epub 2019 Mar 28.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, El-Kasr El-Eini Street, P.O. Box 11562, Cairo, Egypt.

Various pyridopyridazinone derivatives were designed as Poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. The pyridopyridazinone scaffold was used as an isostere of the phthalazine nucleus of the lead compound Olaparib in addition to some modifications in the tail part of the molecule. Preliminary biological evaluation indicated that most compounds possessed inhibitory potencies comparable to Olaparib in nanomolar level. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.068DOI Listing

In vitro and in silico studies of novel synthetic ACE-inhibitory peptides derived from Saccharomyces cerevisiae protein hydrolysate.

Bioorg Chem 2019 Mar 28;87:647-654. Epub 2019 Mar 28.

Department of Biotechnology, Iranian Research Organization for Science & Technology (IROST), Tehran, Iran.

The structure-function relation of YR-10 (YGKPVAVPAR) was investigated by synthesizing four structural analogs of that including YHR-10 (YGKHVAVHAR), GA-8 (GKPVAVPA), GHA-8 (GKHVAVHA), and PAR-3 (PAR). GA-8 (GKPVAVPA) was synthesized on the basis of simulated enzymatic gastrointestinal digestion performed by bioinformatics tools (expasy-peptide cutter). This study explains the molecular mechanisms for the interaction of synthetic peptides with ACE. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.057DOI Listing
March 2019
1 Read

Discovery of new inhibitors against both NF-κB and osteoclastogenesis from in-house library with α, β-unsaturated-enone fragment.

Bioorg Chem 2019 Mar 28;87:638-646. Epub 2019 Mar 28.

Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People's Republic of China; School of Biotechnology and Health Sciences, Wuyi University, 99 Yingbin Road, Jiangmen 529020, People's Republic of China. Electronic address:

The α,β-unsaturated-enone contained natural products have been reported showing NF-κB inhibition effect. It is well known that NF-κB inhibitors can also be used to inhibit osteoclastogenesis. In a continual discovery new agents for anti-osteoclastogenesis, 8 different type compounds with α,β-unsaturated-enone fragments from our in-house library were evaluated for NF-κB inhibition and anti-osteoclastogenesis. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.066DOI Listing

Tick-borne flavivirus reproduction inhibitors based on isoxazole core linked with adamantane.

Bioorg Chem 2019 Mar 16;87:629-637. Epub 2019 Mar 16.

Department of Chemistry, Lomonosov Moscow State University, Leninskie Gory 1 bd. 3, Moscow 119991, Russia; Institute of Physiologically Active Compounds, Severny Proezd 1, Chernogolovka, Moscow Region 142432, Russia. Electronic address:

Infections caused by flaviviruses pose a huge threat for public health all over the world. The search for therapeutically relevant compounds targeting tick-borne flaviviruses requires the exploration of novel chemotypes. In the present work a large series of novel polyfunctionalized isoxazole derivatives bearing substituents with various steric and electronic effects was obtained by our unique versatile synthetic procedure and their antiviral activity against tick-borne encephalitis, Omsk hemorrhagic fever, and Powassan viruses was studied in vitro. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.028DOI Listing
March 2019
4 Reads

New phosphate derivatives of betulin as anticancer agents: Synthesis, crystal structure, and molecular docking study.

Bioorg Chem 2019 Mar 22;87:613-628. Epub 2019 Mar 22.

Medical University of Silesia in Katowice, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, Department of Organic Chemistry, 4 Jagiellońska Str., 41-200 Sosnowiec, Poland.

Betulin derivatives exhibit an antiproliferative activity and have been tested for many cancer cell lines. This paper describes a new series of 3-phosphate derivatives of betulin bearing different substituents at C28 position. The synthesized compounds were tested in vitro for their antiproliferative effect against human leukemia (MV-4-11 and CCRF/CEM), lung carcinoma (A549), prostate cancer (DU 145), melanoma (Hs 294T) cell lines, and murine leukemia P388. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.060DOI Listing
March 2019
1 Read

Synthesis, biological evaluation and molecular modelling studies of 1,3,7,8-tetrasubstituted xanthines as potent and selective A AR ligands with in vivo efficacy against animal model of Parkinson's disease.

Bioorg Chem 2019 Mar 19;87:601-612. Epub 2019 Mar 19.

Institut für Pharmakologie und Toxikologie, Universität Würzburg, Germany.

In the present study, an attempt has been made to develop a new series of 1,3,7,8-tetrasubstituted xanthine based potent and selective AR ligands for the treatment of Parkinson's disease. Antagonistic interactions between dopamine and A adenosine receptors serve as the basis for the development of AR antagonists as potential drug candidates for PD. All the synthesized compounds have been evaluated for their affinity toward AR subtypes using in vitro radioligand binding assays. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.032DOI Listing
March 2019
1 Read

Design, synthesis and evaluation of 2-(indolylmethylidene)-2,3-dihydro-1-benzofuran-3-one and 2-(indolyl)-4H-chromen-4-one derivatives as novel monoamine oxidases inhibitors.

Bioorg Chem 2019 Mar 16;87:594-600. Epub 2019 Mar 16.

Laboratory of Bioorganic Chemistry, Department of Pharmaceutical Sciences, Faculty of Pharmacy and Pharmaceutical Sciences, Josai University, 1-1 Keyaki-dai, Sakado, Saitama 350-0295, Japan.

A series of 2-(indolylmethylidene)-2,3-dihydro-1-benzofuran-3-ones (aurone-indole hybrids) and 2-(indolyl)-4H-chromen-4-ones (flavone-indole hybrids) were designed, synthesized, and their monoamine oxidase (MAO) A and B inhibitory activities were evaluated. Compounds 5b and 11b showed potent inhibitory activities against MAO-A, comparable to that of pargyline used as a positive control, and most of the compounds, except for 2a and 10b, showed potent inhibitory activities against MAO-B. Compound 9a was the most potent and highly selective inhibitor of MAO-B (IC value for MAO-B: 0. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.042DOI Listing

Withanolides from Physalis peruviana showing nitric oxide inhibitory effects and affinities with iNOS.

Bioorg Chem 2019 Mar 22;87:585-593. Epub 2019 Mar 22.

State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300050, People's Republic of China. Electronic address:

A phytochemical study to obtain new nitric oxide (NO) inhibitors resulted in the isolation of five new withanolides from the whole plants of Physalis peruviana. The structures were determined on the basis of extensive NMR spectroscopic data analysis as well as the time-dependent density functional theory (TDDFT) electronic circular dichroism (ECD) calculations. The NO inhibitory effects were examined by inhibiting NO release in lipopolysaccharide-stimulated murine microglial BV-2 cells. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.051DOI Listing
March 2019
2 Reads

Multi-target-directed triazole derivatives as promising agents for the treatment of Alzheimer's disease.

Bioorg Chem 2019 Mar 23;87:572-584. Epub 2019 Mar 23.

Department of Chemistry, Faculty of Basic and Applied Sciences, Sri Guru Granth Sahib World University, Fatehgarh Sahib 140406, Punjab, India. Electronic address:

A novel series of triazole-based compounds have been designed, synthesised and evaluated as multi-target-directed ligands (MTDLs) against Alzheimer disease (AD). The triazole-based compounds have been designed to target four major AD hallmarks that include Aβ aggregation, metal-induced Aβ aggregation, metal dys-homeostasis and oxidative stress. Among the synthesised compounds, 6n having o-CF group on the phenyl ring displayed most potent inhibitory activity (96. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.058DOI Listing
March 2019
11 Reads

Antiproliferative effect, cell cycle arrest and apoptosis generation of novel synthesized anticancer heterocyclic derivatives based 4H-benzo[h]chromene.

Bioorg Chem 2019 Mar 22;87:560-571. Epub 2019 Mar 22.

Chemistry Department, Faculty of Science, Al-Azhar University, Nasr City 11884, Cairo, Egypt.

Novel β-enaminonitrile/ester compounds (4, 6) and an imidate of 4 (9) were utilized as key scaffolds for the synthesis of newly 2-substituted 4H-benzo[h]chromene (7, 8, 10, 11, 13, 14) and 7H-benzo[h]chromeno[2,3-d]pyrimidine derivatives (15-19). The spectral data confirmed the successful isolation of the desired compounds. The targeted compounds were assessed for their in vitro anticancer activity against mammary gland breast cancer cell line (MCF-7), human colon cancer (HCT-116), and liver cancer (HepG-2), while doxorubicin, vinblastine, and colchicine were utilized as standard references drugs. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.059DOI Listing

Synthesis, evaluation and docking of novel pyrazolo pyrimidines as potent p38α MAP kinase inhibitors with improved anti-inflammatory, ulcerogenic and TNF-α inhibitory properties.

Bioorg Chem 2019 Mar 15;87:550-559. Epub 2019 Mar 15.

Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, India. Electronic address:

A series of nine new N-substituted-4-((1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl)amino)benzamides (6a-i) derivatives was synthesized. All the compounds were screened in-vitro for BSA anti-denaturation property, antioxidant assay and p38α MAP kinase inhibition. The in vitro anti-inflammatory assay results revealed that the compounds (6f-i) showed better activity than the compounds 6a-e. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.037DOI Listing

Dual targeting of PTP1B and glucosidases with new bifunctional iminosugar inhibitors to address type 2 diabetes.

Bioorg Chem 2019 Mar 22;87:534-549. Epub 2019 Mar 22.

Department of Experimental and Clinical Biomedical Sciences, University of Florence, Viale Morgagni 50, 50134 Florence, Italy. Electronic address:

The diffusion of type 2 diabetes (T2D) throughout the world represents one of the most important health problems of this century. Patients suffering from this disease can currently be treated with numerous oral anti-hyperglycaemic drugs, but none is capable of reproducing the physiological action of insulin and, in several cases, they induce severe side effects. Developing new anti-diabetic drugs remains one of the most urgent challenges of the pharmaceutical industry. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00452068193007
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http://dx.doi.org/10.1016/j.bioorg.2019.03.053DOI Listing
March 2019
2 Reads

Natural product-based design, synthesis and biological evaluation of 2',3,4,4'-tetrahydrochalcone analogues as antivitiligo agents.

Bioorg Chem 2019 Mar 23;87:523-533. Epub 2019 Mar 23.

State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of TCM Evaluation and Translational Research, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 211198, China. Electronic address:

A bioactive component, 2',3,4,4'-tetrahydrochalcone (RY3-a) was first isolated from Vernohia anthelmintica (L.) willd seeds, and a set of its analogs, RY3-a-1-RY3-a-15 and RY3-c were designed and synthesized. Biological activity assays showed that RY3-c exhibited better melanogenesis and antioxidant activity and lower toxicity in comparison with RY3-a and butin. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.054DOI Listing

Sulfur, selenium and tellurium containing amines act as effective carbonic anhydrase activators.

Bioorg Chem 2019 Mar 25;87:516-522. Epub 2019 Mar 25.

University of Florence, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy. Electronic address:

A new series of β-aminochalcogenides were designed and synthesized to identify new carbonic anhydrase activator (CAA) agents as novel tools for the management of several neurodegenerative and metabolic disorders which represent a clinical challenge without effective therapies available. Some β-aminoselenides and β-aminotellurides showed effective CA activating effects and a potent antioxidant activity. CAAs may have applications for memory therapy and CA deficiency syndromes. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.062DOI Listing

New benzyl pyridinium derivatives bearing 2,4-dioxochroman moiety as potent agents for treatment of Alzheimer's disease: Design, synthesis, biological evaluation, and docking study.

Bioorg Chem 2019 Mar 6;87:506-515. Epub 2019 Mar 6.

Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran. Electronic address:

A new series of benzyl pyridinium-2,4-dioxochroman derivatives 7a-o was synthesized and evaluated as new anti-Alzheimer agents. Among the synthesized compounds, the compounds 7f and 7i exhibited the most potent anti-AChE and anti-BuChE activities, respectively. The kinetic study of the compound 7f revealed that this compound inhibited AChE in a mixed-type inhibition mode. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.012DOI Listing
March 2019
2 Reads

Introduction of amino moiety enhances the inhibitory potency of 1-tetralone chalcone derivatives against LPS-stimulated reactive oxygen species production in RAW 264.7 macrophages.

Bioorg Chem 2019 Mar 20;87:495-505. Epub 2019 Mar 20.

College of Pharmacy, Yeungnam University, Gyeongsan 38541, Republic of Korea. Electronic address:

The design and synthesis of a series of thirty-two halogenated 1-tetralone or 6-amino-1-tetralone chalcone derivatives was achieved by the Claisen-Schmidt condensation reaction and were evaluated for their inhibitory effects against ROS production in LPS-stimulated RAW 264.7 macrophages. It was observed that the introduction of amino moiety into 1-tetralone skeleton greatly increased the inhibitory potency compared to corresponding 1-tetralone chalcones. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.055DOI Listing

Synthesis and biological evaluation of new bisindole-imidazopyridine hybrids as apoptosis inducers.

Bioorg Chem 2019 Mar 22;87:484-494. Epub 2019 Mar 22.

Centre for Semio Chemicals, CSIR-Indian Institute of Chemical Technology (IICT), Hyderabad 500007, India; Academy of Scientific and Innovative Research, New Delhi 110 025, India. Electronic address:

A series of diindolylmethanes (5a-t) were designed, synthesized, and examined for their cytotoxicity against four human cancer cell lines like prostate (DU-145), lung (A549), breast (MCF-7) and cervical cancer (HeLa). These results revealed that among all the hybrids, two (5k and 5r) were identified and exhibited significant cytotoxic effect against A549 cancer cells with IC values of 1.65 ± 0. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.061DOI Listing
March 2019
1 Read
2.152 Impact Factor