37,413 results match your criteria derivatives prepared


Synthesis and biological evaluation of novel isoxazole-piperazine hybrids as potential anti-cancer agents with inhibitory effect on liver cancer stem cells.

Eur J Med Chem 2021 Apr 24;221:113489. Epub 2021 Apr 24.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Ankara, Turkey. Electronic address:

In our effort for the development of novel anticancer therapeutics, a series of isoxazole-piperazine analogues were prepared, and primarily screened for their antiproliferative potential against hepatocellular carcinoma (HCC; Huh7/Mahlavu) and breast (MCF-7) cancer cells. All compounds demonstrated potent to moderate cytotoxicity on all cell lines with IC values in the range of 0.09-11. Read More

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The effect of deoxyfluorination and -acylation on the cytotoxicity of -acetyl-D-gluco- and D-galactosamine hemiacetals.

Org Biomol Chem 2021 May 5. Epub 2021 May 5.

Institute of Chemical Process Fundamentals of the CAS, v. v. i., Rozvojová 135, 16502 Praha 6, Czech Republic.

Fully acetylated deoxyfluorinated hexosamine analogues and non-fluorinated 3,4,6-tri-O-acylated N-acetyl-hexosamine hemiacetals have previously been shown to display moderate anti-proliferative activity. We prepared a set of deoxyfluorinated GlcNAc and GalNAc hemiacetals that comprised both features: O-acylation at the non-anomeric positions with an acetyl, propionyl and butanoyl group, and deoxyfluorination at selected positions. Determination of the in vitro cytotoxicity towards the MDA-MB-231 breast cancer and HEK-293 cell lines showed that deoxyfluorination enhanced cytotoxicity in most analogues. Read More

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Synthesis of cinnamoyl glucoside derivatives and their antiproliferation activities against murine melanoma B16-F10 cell line.

Carbohydr Res 2021 Apr 29;504:108332. Epub 2021 Apr 29.

Food and Pharmacy College, Xuchang University, Xuchang, China. Electronic address:

Twelve cinnamoyl glucoside derivatives were prepared by glycosylation of glucosyl trichloroacetimidate and cinnamic acid derivatives, followed by dechloroacetylation with a pyridine/HO mixture. Their structures were characterized by H and C NMR, as well as mass analysis. All the products were tested for their antiproliferation activities against murine melanoma B16-F10 cell line. Read More

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Torsion-Induced Nonradiative Relaxation of the Singlet Excited State of -Thienyl Bodipy and Charge Separation, Charge Recombination-Induced Intersystem Crossing in Its Compact Electron Donor/Acceptor Dyads.

J Phys Chem B 2021 Apr 30. Epub 2021 Apr 30.

LENS (European Laboratory for Non-Linear Spectroscopy), via N. Carrara 1, 50019 Sesto Fiorentino, Firenze, Italy.

We prepared a series of -thienyl boron-dipyrromethene (Bodipy) derivatives to investigate the spin-orbit charge transfer intersystem crossing (SOCT-ISC). The photophysical properties of the compounds were studied by steady-state and femtosecond/nanosecond transient absorption spectroscopy, as well as density functional theory (DFT) computations. Different from the -phenyl Bodipy analogues, the -thienyl Bodipy are weakly fluorescent. Read More

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Synthesis of Stannylated Aryl Imines and Amines via Aryne Insertion Reactions into Sn-N Bonds.

Chemistry 2021 Apr 30. Epub 2021 Apr 30.

Westfalische Wilhelms-Universitat Munster, Organisch-Chemisches Institut, Corrensstrasse 40, 48149, Münster, GERMANY.

The reaction of in situ generated arynes with stannylated imines to provide ortho -stannyl-aniline derivatives is reported. The readily prepared trimethylstannyl benzophenone imine is introduced as an efficient reagent to realize the aryne σ-insertion reaction. The imine functionality is an established N-protecting group and insertions proceed with good yields and good to excellent regioselectivities. Read More

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Optimized Synthesis of New N-Mustards Based on 2-Mercaptobenzoxazole Derivatives with Antitumor Activity.

Biomedicines 2021 Apr 26;9(5). Epub 2021 Apr 26.

Department of Physiology and Pathophysiology, Faculty of Veterinary Medicine, "Ion Ionescu de la Brad" University of Agricultural Sciences and Veterinary Medicine, 700490 Iasi, Romania.

New di-(β-chloroethyl)-amides of some acids derived from 2-mercaptobenzoxazole were prepared by reaction of the corresponding pivalic mixed anhydrides with di-(β-chloroethyl)-amine. A study regarding the optimization of the chemical reactions was made for the case of di-(β-chloroethyl)-amines. The quantum chemical analysis by Spartan'14 was made in order to establish the most stable configuration of the ground electronic states for the obtained chemical structures and some physico-chemical parameters of N-mustards reported in this paper. Read More

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New Acyl Derivatives of 3-Aminofurazanes and Their Antiplasmodial Activities.

Pharmaceuticals (Basel) 2021 Apr 27;14(5). Epub 2021 Apr 27.

Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstraße 1, A-8010 Graz, Austria.

An -acylated furazan-3-amine of a Medicines for Malaria Venture (MMV) project has shown activity against different strains of . Seventeen new derivatives were prepared and tested in vitro for their activities against blood stages of two strains of . Several structure-activity relationships were revealed. Read More

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Schrenk from Kazakhstan-Natural Source of Bioactive Compounds with Cosmetic Significance.

Molecules 2021 Apr 28;26(9). Epub 2021 Apr 28.

Independent Laboratory of Natural Products Chemistry, Department of Pharmacognosy, Medical University of Lublin, 1 Chodzki Str., 20-093 Lublin, Poland.

Plants belonging to the genus are known for their high content of bioactive molecules and broad spectrum of healing and cosmetic activities.  Schrenk is a wild-type species abundant in the mountainous regions of Kazakhstan. The phytochemical composition as well as the bioactivity of  extracts have not been fully investigated to date. Read More

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Design and Gas Separation Performance of Imidazolium Poly(ILs) Containing Multivalent Imidazolium Fillers and Crosslinking Agents.

Polymers (Basel) 2021 Apr 24;13(9). Epub 2021 Apr 24.

Department of Chemical & Biological Engineering, University of Alabama, Tuscaloosa, AL 35487-0203, USA.

This work introduces a series of vinyl-imidazolium-based polyelectrolyte composites, which were structurally modified via impregnation with multivalent imidazolium-benzene ionic liquids (ILs) or crosslinked with novel cationic crosslinkers which possess internal imidazolium cations and vinylimidazolium cations at the periphery. A set of eight [Cvim][TfN]-based membranes were prepared via UV-initiated free radical polymerization, including four composites containing di-, tri-, tetra-, and hexa-imidazolium benzene ILs and four crosslinked derivatives which utilized tri- and tetra- vinylimidazolium benzene crosslinking agents. Structural and functional characterizations were performed, and pure gas permeation data were collected to better understand the effects of "free" ILs dispersed in the polymeric matrix versus integrated ionic crosslinks on the transport behaviors of these thin films. Read More

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Evaluation of Chitosan Derivatives Modified Mesoporous Silica Nanoparticles as Delivery Carrier.

Molecules 2021 Apr 24;26(9). Epub 2021 Apr 24.

Key Laboratory of Chemical Engineering Process and Technology for High-efficiency Conversion, College of Chemistry and Material Sciences, Heilongjiang University, Harbin 150080, China.

Chitosan is a non-toxic biological material, but chitosan is insoluble in water, which hinders the development and utilization of chitosan. Chitosan derivatives -2-Hydroxypropyl trimethyl ammonium chloride (-2-HACC) and carboxymethyl chitosan (CMCS) with good water solubility were synthesized by our laboratory. In this study, we synthesized mesoporous SiO nanoparticles by the emulsion, and then the mesoporous SiO nanoparticles were modified with γ-aminopropyltriethoxysilane to synthesize aminated mesoporous SiO nanoparticles; CMCS and -2-HACC was used to cross-link the aminated mesoporous SiO nanoparticles to construct SiO@CMCS--2-HACC nanoparticles. Read More

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Combining Dextran Conjugates with Stimuli-Responsive and Folate-Targeting Activity: A New Class of Multifunctional Nanoparticles for Cancer Therapy.

Nanomaterials (Basel) 2021 Apr 25;11(5). Epub 2021 Apr 25.

Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Italy.

Nanoparticles with active-targeting and stimuli-responsive behavior are a promising class of engineered materials able to recognize the site of cancer disease, targeting the drug release and limiting side effects in the healthy organs. In this work, new dual pH/redox-responsive nanoparticles with affinity for folate receptors were prepared by the combination of two amphiphilic dextran (DEX) derivatives. DEXFA conjugate was obtained by covalent coupling of the polysaccharide with folic acid (FA), whereas DEXssPEGCOOH derived from a reductive amination step of DEX was followed by condensation with polyethylene glycol 600. Read More

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New Bioconjugated Technetium and Rhenium Folates Synthesized by Transmetallation Reaction with Zinc Derivatives.

Molecules 2021 Apr 19;26(8). Epub 2021 Apr 19.

Unitat de Biofísica/Centre d'Estudis en Biofísica, Facultat de Medicina, Departament de Bioquímica i Biologia Molecular, Universitat Autònoma de Barcelona, 08193 Cerdanyola del Vallès, Catalonia, Spain.

The zinc dithiocarbamates functionalized with folic acid and were synthesized with a simple straightforward method, using an appropriated folic acid derivative and a functionalized zinc dithiocarbamate (). Zinc complexes and show very low solubilities in water, making them useful for preparing Tc-99m radiopharmaceuticals with a potentially high molar activity. Thus, the transmetallation reaction in water medium between the zinc complexes or and the cation -[Tc(HO)(CO)], in the presence of the monodentate ligand TPPTS, leads to the formation of the 2 + 1 complexes -[Tc(CO)(SS)(P)] bioconjugated to folic acid ( and ). Read More

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Synthesis and Single Crystal Structures of -Substituted Benzamides and Their Chemoselective Selenation/Reduction Derivatives.

Molecules 2021 Apr 19;26(8). Epub 2021 Apr 19.

EaStCHEM School of Chemistry, University of St Andrews, St Andrews Fife KY16 9ST, UK.

A series of -aryl--(2-oxo-2-arylethyl) benzamides and cinnamides has been prepared. The reaction of the benzamides with Woollins' reagent, a highly efficient chemoselective selenation/reduction reagent, gave the corresponding -aryl--(arylenethyl) benzoselenoamides in good yields. Five representative single crystal X-ray structures are discussed. Read More

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Hybrid Materials Based on Magnetic Iron Oxides with Benzothiazole Derivatives: A Plausible Potential Spectroscopy Probe.

Int J Mol Sci 2021 Apr 12;22(8). Epub 2021 Apr 12.

Department of Chemistry, Federal University of Lavras, No 37, Lavras 37200-900, MG, Brazil.

Rare diseases affect a small part of the population, and the most affected are children. Because of the low availability of patients for testing, the pharmaceutical industry cannot develop drugs for the diagnosis of many of these orphan diseases. In this sense, the use of benzothiazole compounds that are highly selective and can act as spectroscopy probes, especially the compound 2-(4'-aminophenyl)benzothiazole (ABT), has been highlighted. Read More

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Dual-Target Compounds against Type 2 : Proof of Concept for Sodium Dependent Glucose Transporter (SGLT) and Glycogen Phosphorylase (GP) Inhibitors.

Pharmaceuticals (Basel) 2021 Apr 15;14(4). Epub 2021 Apr 15.

Department of Organic Chemistry, University of Debrecen, POB 400, H-4002 Debrecen, Hungary.

A current trend in the quest for new therapies for complex, multifactorial diseases, such as diabetes mellitus (DM), is to find dual or even multi-target inhibitors. In DM, the sodium dependent glucose cotransporter 2 (SGLT2) in the kidneys and the glycogen phosphorylase (GP) in the liver are validated targets. Several (β-D-glucopyranosylaryl)methyl (het)arene type compounds, called gliflozins, are marketed drugs that target SGLT2. Read More

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Use of Pluronic Surfactants in Gel Formulations of Photosensitive 1,4-Dihydropyridine Derivatives: A Potential Approach in the Treatment of Neuropathic Pain.

Pharmaceutics 2021 Apr 10;13(4). Epub 2021 Apr 10.

Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Italy.

1,4-Dihydropyridines (DHPs) are the most important class of L-type calcium channel blockers that are employed for the treatment of cardiovascular diseases, particularly hypertension. Various modifications on this scaffold lead to the discovery of new DHPs blocking different types of calcium channels. Among them, the T-type calcium channel has recently attracted great interest due to its role in chronic pain conditions. Read More

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Comparison of the Benzanthrone Luminophores: They Are Not Equal for Rapid Examination of (Trematoda: Digenea).

Biomolecules 2021 Apr 18;11(4). Epub 2021 Apr 18.

Institute of Life Sciences and Technology, Daugavpils University, Parades Street 1A, LV-5401 Daugavpils, Latvia.

Luminescent derivatives of benzanthrone are becoming more useful based on their light-absorbing and fluorescent-emitting properties. Our previous studies showed that luminescent staining properties of the same benzanthrone dye differ for variable parasite samples. Therefore, two types of benzanthrone dyes were prepared. Read More

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Inhibitory Effects of Erythrosine/Curcumin Derivatives/Nano-Titanium Dioxide-Mediated Photodynamic Therapy on .

Molecules 2021 Apr 21;26(9). Epub 2021 Apr 21.

Laser in Dentistry Research Group, Khon Kaen University, Khon Kaen 40002, Thailand.

This study focuses on the role of photosensitizers in photodynamic therapy. The photosensitizers were prepared in combinations of 110/220 µM erythrosine and/or 10/20 µM demethoxy/bisdemethoxy curcumin with/without 10% () nano-titanium dioxide. Irradiation was performed with a dental blue light in the 395-480 nm wavelength range, with a power density of 3200 mW/cm and yield of 72 J/cm. Read More

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Synthesis, Mesomorphic and Computational Characterizations of Nematogenic Schiff Base Derivatives in Pure and Mixed State.

Molecules 2021 Apr 2;26(7). Epub 2021 Apr 2.

Chemistry Department, College of Sciences, Yanbu, Taibah University, Yanbu 30799, Saudi Arabia.

Homolog series based on three aromatic rings bearing terminal alkoxy chain of various lengths named 4-(4-(alkoxy)phenylimino)methyl)phenyl nicotinate () were synthesized. The alkoxy-chain length changed between 6, 8 and 16 carbons. Mesomorphic and optical properties were carried out via differential scanning calorimetry (DSC) and polarized optical microscopy (POM). Read More

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Electrodeposited Copolymers Based on 9,9'-(5-Bromo-1,3-phenylene)biscarbazole and Dithiophene Derivatives for High-Performance Electrochromic Devices.

Polymers (Basel) 2021 Apr 2;13(7). Epub 2021 Apr 2.

Department of Chemical Engineering and Materials Engineering, National Yunlin University of Science and Technology, Yunlin 64002, Taiwan.

A 1,3-bis(carbazol-9-yl)benzene derivative (BPBC) was synthesized and its related homopolymer (PBPBC) and copolymers (P(BPBC--BT), P(BPBC--CDT), and P(BPBC--CDTK)) were prepared using electrochemical polymerization. Investigations of polymeric spectra showed that PBPBC film was grey, iron-grey, yellowish-grey, and greyish-green from the neutral to the oxidized state. P(BPBC--BT), P(BPBC--CDT), and P(BPBC--CDTK) films showed multicolor transitions from the reduced to the oxidized state. Read More

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Novel Ring Systems: Spiro[Cycloalkane] Derivatives of Triazolo- and Tetrazolo-Pyridazines.

Molecules 2021 Apr 8;26(8). Epub 2021 Apr 8.

Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, H-1111 Budapest, Hungary.

In orderto synthesize new pyridazine derivatives anellated with different nitrogen heterocyclic moieties, spiro[cycloalkane]pyridazinones were transformed into the corresponding thioxo derivatives via a reaction with phosphorus pentasulfide. The reaction of the formed 2,3-diazaspiro[5.5] undec-3-ene-1-thiones with hydrazine provided the corresponding 1-hydrazono-2,3-diazaspiro[5. Read More

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Multidimensional Ln-Aminophthalate Photoluminescent Coordination Polymers.

Materials (Basel) 2021 Apr 4;14(7). Epub 2021 Apr 4.

LAQV/REQUIMTE & Department of Chemistry and Biochemistry, Faculty of Sciences, University of Porto, 4169-007 Porto, Portugal.

The development of straightforward reproducible methods for the preparation of new photoluminescent coordination polymers (CPs) is an important goal in luminescence and chemical sensing fields. Isophthalic acid derivatives have been reported for a wide range of applications, and in addition to their relatively low cost, have encouraged its use in the preparation of novel lanthanide-based coordination polymers (LnCPs). Considering that the photoluminescent properties of these CPs are highly dependent on the existence of water molecules in the crystal structure, our research efforts are now focused on the preparation of CP with the lowest water content possible, while considering a green chemistry approach. Read More

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Acetalated dextran based nano- and microparticles: synthesis, fabrication, and therapeutic applications.

Chem Commun (Camb) 2021 Apr;57(35):4212-4229

Drug Research Program, Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmacy, University of Helsinki, FI-00014 Helsinki, Finland. and Helsinki Institute of Life Science (HiLIFE), University of Helsinki, FI-00014 Helsinki, Finland.

Acetalated dextran (Ac-DEX) is a pH-responsive dextran derivative polymer. Prepared by a simple acetalation reaction, Ac-DEX has tunable acid-triggered release profile. Despite its relatively short research history, Ac-DEX has shown great potential in various therapeutic applications. Read More

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Automated Radiosynthesis of - and -4-[F]Fluoro-l-proline Using [F]Fluoride.

J Org Chem 2021 Apr 29. Epub 2021 Apr 29.

WestCHEM, School of Chemistry, University of Glasgow, The Joseph Black Building, Glasgow G12 8QQ, United Kingdom.

The positron emission tomography imaging agents - and -4-[F]fluoro-l-proline are used for the detection of numerous diseases such as pulmonary fibrosis and various carcinomas. These imaging agents are typically prepared by nucleophilic fluorination of 4-hydroxy-l-proline derivatives, with [F]fluoride, followed by deprotection. Although effective radiofluorination reactions have been developed, the overall radiosynthesis process is suboptimal due to deprotection methods that are performed manually, require multiple steps, or involve harsh conditions. Read More

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A photostable reaction-based A-A-A type two-photon fluorescent probe for rapid detection and imaging of sulfur dioxide.

J Mater Chem B 2021 Apr;9(16):3554-3562

Laboratory of Functionalized Molecular Solids, Ministry of Education, Anhui Key Laboratory of Chemo/Biosensing, Laboratory of Biosensing and Bioimaging (LOBAB), College of Chemistry and Materials Science, Anhui Normal University, Wuhu 241002, P. R. China.

In this study, a novel reaction-based A-A-A (acceptor-acceptor-acceptor) type two-photon fluorescent probe, BTC, is prepared using the benzothiadiazole (BTD) scaffold as the two-photon fluorophore and electron-accepting centre. Two β-chlorovinyl aldehyde moieties are symmetrically connected to both ends of the BTD scaffold and act as reaction groups to recognize SO2 and quenching groups to make the dis-activated probe stay at off-state due to their weak electron-withdrawing effect. In the presence of SO2 derivatives, the aldehyde groups are consumed through aldehyde addition, resulting in the activation of intramolecular charge transfer (ICT) processes and therefore recovering the fluorescence of the probe. Read More

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Palladium oxide-decorated mesoporous silica on graphene oxide nanosheets as a heterogeneous catalyst for the synthesis of β-substituted indole derivatives.

Dalton Trans 2021 Apr;50(16):5644-5658

Department of Chemistry, University of Delhi, Delhi-110007, India.

In this work, an efficient and facile strategy has been adopted for the stepwise synthesis of the RGO-MSiO2/PdO hybrid nanomaterial (HY-NM). Herein, a hybrid nanostructure of mesoporous silica over graphene oxide (GO) sheets has been developed followed by immobilizing palladium oxide nanoparticles (PdO NPs), and then it has been utilized for catalyzing a multicomponent reaction (MCR). To authenticate the successful synthesis of the HY-NM and successive immobilization of PdO NPs, various physicochemical characterization techniques were utilized such as SEM, EDAX, HR-TEM, HR-XRD, TGA, BET, FT-IR, and XPS analysis. Read More

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A Structure-Activity Relationship Study of Bimodal BODIPY-labeled PSMA-targeting Bioconjugates.

ChemMedChem 2021 Apr 27. Epub 2021 Apr 27.

Saarland University - Medical Center, Nuklearmedizin, Kirrbergerstrasse, 66421, Homburg, GERMANY.

The aim of the study was to identify a high affinity BODIPY peptidomimetic targeting the prostate specific membrane antigen (PSMA) as potential bimodal imaging probe for prostate cancer. For the structure-activity study, several BODIPY derivatives with varying spacers between the BODIPY dye and the PSMA Glu-CO-Lys binding motif were prepared. Corresponding affinities were determined by competitive binding assays in PSMA-positive LNCaP cells. Read More

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Synthesis of oxadiazole-2-oxide derivatives as potential drug candidates for schistosomiasis targeting SjTGR.

Parasit Vectors 2021 Apr 26;14(1):225. Epub 2021 Apr 26.

School of Life Science and Engineering, Southwest University of Science and Technology, Mianyang, 621010, China.

Background: Schistosomiasis is a chronic parasitic disease that affects millions of people's health worldwide. Because of the increasing drug resistance to praziquantel (PZQ), which is the primary drug for schistosomiasis, developing new drugs to treat schistosomiasis is crucial. Oxadiazole-2-oxides have been identified as potential anti-schistosomiasis reagents targeting thioredoxin glutathione reductase (TGR). Read More

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Discovery of boronic acid-based potent activators of tumor pyruvate kinase M2 and development of gastroretentive nanoformulation for oral dosing.

Bioorg Med Chem Lett 2021 Apr 23:128062. Epub 2021 Apr 23.

Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research-Ahmedabad, India. Electronic address:

Several studies have established that cancer cells explicitly over-express the less active isoform of pyruvate kinase M2 (PKM2) is critical for tumorigenesis. The activation of PKM2 towards tetramer formation may increase affinity towards phosphoenolpyruvate (PEP) and avoidance of the Warburg effect. Herein, we describe the design, synthesis, and development of boronic acid-based molecules as activators of PKM2. Read More

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Copper-catalyzed [3 + 2]-cycloaddition of α-halonitroalkenes with azomethine ylides: facile synthesis of multisubstituted pyrrolidines and pyrroles.

Org Biomol Chem 2021 Apr;19(15):3413-3427

N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Leninsky prosp. 47, Moscow, 119991, Russia.

An efficient route for the synthesis of multifunctionalized pyrrolidines based on copper-catalyzed diastereoselective [3 + 2]-cycloaddition of nitroalkenes with azomethine ylides was developed. Novel fluorinated heterocycles - β-fluoro-β-nitropyrrolidines - were accessed via this method. The products can be prepared in good to excellent yields and with high diastereoselectivity. Read More

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