35,184 results match your criteria revealed synthesized


Substituted dienes prepared from betulinic acid - Synthesis, cytotoxicity, mechanism of action, and pharmacological parameters.

Eur J Med Chem 2021 Jul 15;224:113706. Epub 2021 Jul 15.

Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University Olomouc, Hněvotínská 1333/5, 779 00, Olomouc, Czech Republic. Electronic address:

A set of new substituted dienes were synthesized from betulinic acid by its oxidation to 30-oxobetulinic acid followed by the Wittig reaction. Cytotoxicity of all compounds was tested in vitro in eight cancer cell lines and two noncancer fibroblasts. Almost all dienes were more cytotoxic than betulinic acid. Read More

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Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.

Eur J Med Chem 2021 Jul 15;224:113700. Epub 2021 Jul 15.

Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China; Pharmacy Department, Zhujiang Hospital, Southern Medical University, Guangzhou, 510515, China. Electronic address:

To discover PDE4/tubulin dual inhibitors with novel skeleton structures, 7-trimethoxyphenylbenzo[d]oxazoles 4a-u and 4-trimethoxyphenylbenzo[d]oxazoles 5a-h were designed and synthesized by migrating the trimethoxyphenyl group of TH03 to the benzo[d]oxazole moiety. Among these compounds, approximately half of them displayed good antiproliferative activities against glioma (U251) and lung cancer (A549 and H460) cell lines. The structure-activity relationships of trimethoxyphenylbenzo[d]oxazoles led to the identification of 4r bearing indol-5-yl side-chain as a novel dual PDE4/tubulin inhibitor, which exhibited satisfactory antiproliferative activities against glioma (IC = 300 ± 50 nM) and lung cancer (average IC = 39. Read More

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Precursor effects on the physical, biological, and catalytic properties of Fagonia indica Burm.f. mediated zinc oxide nanoparticles.

Microsc Res Tech 2021 Jul 26. Epub 2021 Jul 26.

Department of Plant Sciences, Quaid-i-Azam University, Islamabad, Pakistan.

We report a facile, green and precursor-based comparative study on the biosynthesis of zinc oxide (ZnO) nanoparticles (NPs) using anticancerous Fagonia indica as effective chelating agent. Biosynthesis was carried out using zinc sulfate and zinc acetate as precursor salts to make ZnO and ZnO NPs under similar experimental conditions which were characterized extensively for physical and biological properties. Scherrer equation deduced a mean crystallite size of ~23. Read More

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Fragmenlt Recombination Design, Synthesis, and Safener Activity of Novel Ester-Substituted Pyrazole Derivatives.

J Agric Food Chem 2021 Jul 26. Epub 2021 Jul 26.

Department of Chemistry, College of Arts and Sciences, Northeast Agricultural University, Harbin 150030, China.

Fenoxaprop--ethyl (FE), a type of acetyl-CoA carboxylase (ACCase) inhibitor, has been extensively applied to a variety of crop plants. It can cause damage to wheat () even resulting in the death of the crop. On the prerequisite of not reducing herbicidal efficiency on target weed species, herbicide safeners selectively protect crops from herbicide injury. Read More

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Transcriptome and proteome dynamics of cervical remodeling in the mouse during pregnancy.

Biol Reprod 2021 Jul 26. Epub 2021 Jul 26.

Department of Ob/Gyn and Cecil H. and Ida Green Center for Reproductive Biological Science, The University of Texas Southwestern Medical Center, Dallas, TX.

During gestation, the female reproductive tract must maintain pregnancy while concurrently preparing for parturition. Here, we explore the transitions in gene expression and protein turnover (fractional synthesis rates [FSR]) by which the cervix implements a transition from rigid to compliant. Shifts in gene transcription to achieve immune tolerance and alter epithelial cell programs begin in early pregnancy. Read More

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Characterization of different oligomeric forms of CRISP2 in the perinuclear theca versus the fibrous tail structures of boar spermatozoa.

Biol Reprod 2021 Jul 26. Epub 2021 Jul 26.

Department of Biomolecular Health Sciences, Faculty of Veterinary Medicine, Utrecht University, the Netherlands.

Mammalian sperm carry a variety of highly condensed insoluble protein structures such as the perinuclear theca, the fibrous sheath and the outer dense fibers, which are essential to sperm function. We studied the role of cysteine rich secretory protein 2 (CRISP2); a known inducer of non-pathological protein amyloids, in pig sperm with a variety of techniques. CRISP2, which is synthesized during spermatogenesis, was localized by confocal immunofluorescent imaging in the tail and in the post-acrosomal region of the sperm head. Read More

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Spatial Control of Dynamic Junctions in Transition Metal Dichalcogenide Light-Emitting Devices.

ACS Nano 2021 Jul 26. Epub 2021 Jul 26.

Department of Applied Physics, Nagoya University, Nagoya 464-8603, Japan.

Emerging transition metal dichalcogenides (TMDCs) offer an attractive platform for investigating functional light-emitting devices, such as flexible devices, quantum and chiral devices, high-performance optical modulators, and ultralow threshold lasers. In these devices, the key operation is to control the light-emitting position, that is, the spatial position of the recombination zone to generate electroluminescence, which permits precise light guides/passes/confinement to ensure favorable device performance. Although various structures of TMDC light-emitting devices have been demonstrated, including the transistor configuration and heterostructured diodes, it is still difficult to tune the light-emitting position precisely owing to the structural device complexity. Read More

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Ferrous ions doped layered double hydroxide: smart 2D nanotheranostic platform with imaging-guided synergistic chemo/photothermal therapy for breast cancer.

Biomater Sci 2021 Jul 26. Epub 2021 Jul 26.

Key Laboratory of Advanced Materials, Ministry of Education of China, School of Materials Science and Engineering, Tsinghua University, Beijing 100084, China and State Key Laboratory of New Ceramics and Fine Processing, School of Materials Science and Engineering, Tsinghua University, Beijing 100084, China.

Developing simple and efficient nanotheranostic platforms with behavior responsive to the acid microenvironment of a tumor is of great significance for accurate tumor diagnosis and therapy. In this study, a smart 2D nanotheranostic platform has been successfully fabricated by doping functional ferrous ions into as-synthesized MgAl-layered double hydroxide (LDH) with doxurubicin (DOX) loading to form Fe-LDH/DOX NPs, which achieved magnetic resonance imaging (MRI)-guided synergistic chemo/photothermal therapy for breast cancer. The doping of ferrous ions into Fe-LDH/DOX enabled a strong photo-induced heating ability with a high photothermal conversion efficiency of 45. Read More

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TiO-Doped NiCuZnFeO Nanoparticles for Enhanced Structural and Magnetic Properties.

ACS Omega 2021 Jul 9;6(28):17931-17940. Epub 2021 Jul 9.

Solid State Physics Division, Bhabha Atomic Research Centre, Mumbai 400085, Maharashtra, India.

TiO (0-10 wt %)-doped nanocrystalline NiCuZnFeO (Ni-Cu-Zn) ferrites were synthesized using the sol-gel route of synthesis. The cubic spinel structure of the ferrites having the 3 space group was revealed from the analysis of Rietveld refined X-ray diffraction (XRD) data. The secondary phase of TiO with a space group of 41/ was observed within the ferrites with doping, > 3 wt %. Read More

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The Assessment of Pentraxin 3: A Novel Biomarker in Early Detection of Infection in Newborns.

Biomed Res Int 2021 30;2021:6638622. Epub 2021 Jun 30.

Department of Neonatology, Faculty of Medical Sciences in Katowice, Medical University of Silesia in Katowice, Poland.

Introduction: As the clinical manifestation of neonatal infection is nonspecific and characterised by varied clinical features, it is highly problematic to establish an early diagnosis. Recently, hopes have been raised by the new acute-phase protein-pentraxin 3 (PTX3). PTX3 belongs to the family of long pentraxins, which is synthesized in numerous cells like endothelial cells, macrophages, and monocytes infiltrating sites of inflammation. Read More

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Starch Nanoparticles for Enhancement of Oral Bioavailability of a Newly Synthesized Thienopyrimidine Derivative with Anti-Proliferative Activity Against Pancreatic Cancer.

Drug Des Devel Ther 2021 16;15:3071-3093. Epub 2021 Jul 16.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt.

Purpose: This research aimed to improve water solubility and oral bioavailability of a newly synthesized thienopyrimidine derivative (TPD) with anti-pancreatic cancer activity by loading on starch nanoparticles (SNPs).

Methods: TPD was synthesized, purified and its ADME behavior was predicted using Swiss ADME software. A UV spectroscopy method was developed and validated to measure TPD concentration at various dosage forms. Read More

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Sulfation of chitosan from as potential anticoagulant and antibacterial molecule.

Nat Prod Res 2021 Jul 24:1-7. Epub 2021 Jul 24.

Department of Pharmacology & Toxicology, College of Pharmacy (Girls), Prince Sattam Bin Abdul Aziz University, Al-Kharj, Saudi Arabia.

The present work aimed to synthesis of chitin, chitosan and sulfation of chitosan from cuttlebone of cuttlefish . Principally chitin was extracted through sequential processes of demineralisation and deproteinzation. Then chitosan was synthesized by a deacetylation and finally sulfated at semi-heterogeneous condition using chlorosulfonic acid in ,-dimethylformamide. Read More

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Magnetic nanostructured lipid carrier for dual triggered curcumin delivery: Preparation, characterization and toxicity evaluation on isolated rat liver mitochondria.

J Biomater Appl 2021 Jul 26:8853282211034625. Epub 2021 Jul 26.

Department of Pharmaceutical Biomaterials, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran.

In this research, magnetic nanostructured lipid carriers (Mag-NLCs) were synthesized for curcumin (CUR) delivery. NLCs are drug-delivery systems prepared by mixing solid and liquid (oil) lipids. For preparation of NLCs, cetylpalmitate was selected as solid lipid and fish oil as liquid lipid. Read More

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Design, synthesis and evaluation of tetrahydrocarbazole derivatives as potential hypoglycemic agents.

Bioorg Chem 2021 Jul 17;115:105172. Epub 2021 Jul 17.

State Key Laboratory of Functions and Applications of Medicinal Plants & College of Pharmacy, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Medical University, Guiyang 550004, China. Electronic address:

Two series of tetrahydrocarbazole derivatives have been designed and synthesized based on ZG02, a promising candidate developed in our previous studies. The newly prepared compounds were screened for glucose consumption activity in HepG2 cell lines. Aza-tetrahydrocarbazole compound 12b showed the most potent hypoglycemic activity with a 45% increase in glucose consumption when compared to the solvent control, which had approximately 1. Read More

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Novel halogenated arylvinyl-1,2,4 trioxanes as potent antiplasmodial as well as anticancer agents: Synthesis, bioevaluation, structure-activity relationship and in-silico studies.

Eur J Med Chem 2021 Jul 10;224:113685. Epub 2021 Jul 10.

Laboratory of Organic and Medicinal Chemistry, Department of Chemistry, Malaviya National Institute of Technology, Jawaharlal Nehru Marg, Jaipur, 302017, India; Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research-Raebareli (Transit Campus), Bijnor-Sisendi Road, Near CRPF Base Camp, Sarojini Nagar, Lucknow, U.P, 226 002, India. Electronic address:

Herein, we have synthesized a series of lipophilic, halogenated-arylvinyl-1,2,4-trioxanes 8a-g (28 compounds) and assessed for their in vitro anti-plasmodial activity in Plasmodium falciparum culture using SYBRgreen-I fluorescence assay against chloroquine-resistant Pf INDO and artemisinin-resistant Pf Cam 3.1 (MRA-1240) strains. Alongside, the cell cytotoxic potential of 8a-g has also been determined against the HEK293 cell line in vitro. Read More

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Hdpa derivatives containing pentadentate ligands: An acyclic adjuvant potentiates meropenem activity in vitro and in vivo against metallo-β-lactamase-producing Enterobacterales.

Eur J Med Chem 2021 Jul 13;224:113702. Epub 2021 Jul 13.

School of Pharmaceutical Sciences, Institute of Drug Discovery and Development, Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Zhengzhou University, Zhengzhou, 450001, PR China. Electronic address:

The emergence and dissemination of metallo-β-lactamases (MBLs) producing Enterobacterales is a great concern for public health due to the limited therapeutic options. No MBL inhibitors are currently available in clinical practice. Herein, we synthesized a series of Hdpa derivatives containing pentadentate-chelating ligands and evaluated their inhibitory activity against MBLs. Read More

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Cytotoxic oxidovanadium(IV) complexes of tridentate halogen-substituted Schiff bases: First dinuclear V(IV) complexes with O→V=O→V=O core.

Bioorg Med Chem Lett 2021 Jul 22:128285. Epub 2021 Jul 22.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences,University of Messina, Viale Ferdinando Stagno D'Alcontres 31, I-98166 Messina, Italy.

The reaction of potentially N,N,O-tridentate Schiff base ligands, Cl-LH, Br-LH, BrCl-LH and H-LH, with [VO(acac)] in 2:1 molar ratio in methanol gave the corresponding mononuclear and dinuclear oxidovanadium(IV) complexes, VO(Cl-L) (1), VO(Br-L) (2), [(BrCl-L)(HO)V(μ-O)VO(BrCl-L)] (3) and [(H-L)(HO)V(μ -O)VO(H-L)] (4), in good yields. The ligands and complexes were fully characterized by elemental analysis and FT-IR spectroscopy. The ligands were also characterized by H NMR spectroscopy. Read More

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Pre-loss grief and preparedness for death among caregivers of terminally ill cancer patients: A systematic review.

Soc Sci Med 2021 Jul 19;284:114240. Epub 2021 Jul 19.

Department of Psychosomatic Medicine and Psychotherapy, University of Leipzig, Semmelweisstraße 10, 04103, Leipzig, Germany. Electronic address:

Background: Cancer is one of the most common causes of death. The period of time between receiving a terminal diagnosis of cancer and the death of a loved one has been operationalized as pre-loss grief and, more recently, as preparedness for death. Originally, grief before loss was thought to have positive effects on the bereavement outcome, but some studies have revealed contradictory findings. Read More

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Phenoxypyridine derivatives containing natural product coumarins with allelopathy as novel and promising proporphyrin IX oxidase-inhibiting herbicides: Design, synthesis and biological activity study.

Pestic Biochem Physiol 2021 Aug 9;177:104897. Epub 2021 Jun 9.

Department of Chemistry, College of Arts and Sciences, Northeast Agricultural University, Harbin 150030, China. Electronic address:

To seek novel and safe protoporphyrinogen oxidase (PPO, EC 1.3.3. Read More

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Preparation, Characterization, and Evaluation of Macrocrystalline and Nanocrystalline Cellulose as Potential Corrosion Inhibitors for SS316 Alloy during Acid Pickling Process: Experimental and Computational Methods.

Polymers (Basel) 2021 Jul 12;13(14). Epub 2021 Jul 12.

Department of Chemistry, College of Science, King Faisal University, Al Hofuf, Al-Ahsa 31982, Saudi Arabia.

Converting low-cost bio-plant residuals into high-value reusable nanomaterials such as microcrystalline cellulose is an important technological and environmental challenge. In this report, nanocrystalline cellulose (NCC) was prepared by acid hydrolysis of macrocrystalline cellulose (CEL). The newly synthesized nanomaterials were fully characterized using spectroscopic and microscopic techniques including FE-SEM, FT-IR, TEM, Raman spectroscopy, and BET surface area. Read More

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Preparation of Colored Microcapsule Phase Change Materials with Colored SiO Shell for Thermal Energy Storage and Their Application in Latex Paint Coating.

Materials (Basel) 2021 Jul 18;14(14). Epub 2021 Jul 18.

College of Materials Science and Engineering, Zhejiang University of Technology, Hangzhou 310000, China.

This article reports the design and manufacture of colored microcapsules with specific functions and their application in architectural interior wall coating. Utilizing reactive dyes grafted SiO shell to encapsulate paraffin through interfacial polymerization and chemical grafting methods, this experiment successfully synthesized [email protected] colored microcapsules. The observations of surface morphology demonstrated that the colored microcapsules had a regular spherical morphology and a well-defined core-shell structure. Read More

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Synthesis, Biological and In Silico Studies of a Tripodal Schiff Base Derived from 2,4,6-Triamino-1,3,5-triazine and Its Trinuclear Dy(III), Er(III), and Gd(III) Salen Capped Complexes.

Molecules 2021 Jul 20;26(14). Epub 2021 Jul 20.

Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka 410001, Nigeria.

A tripodal Schiff base ligand, 2,4,6-Tris(4-carboxybenzimino)-1,3,5-triazine (MT) and its trinuclear Dy(III), Er(III), and Gd(III) complexes were synthesized. These were characterized using UV-visible, IR, H, and C NMR spectroscopies, elemental analysis, and molar conductivity measurements. The spectral studies indicate that the ligand is hexadentate and coordinates to the Ln(III) ions through the oxygen atoms of the carboxylic group. Read More

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Label-Free Electrochemical Sensor Based on Manganese Doped Titanium Dioxide Nanoparticles for Myoglobin Detection: Biomarker for Acute Myocardial Infarction.

Molecules 2021 Jul 13;26(14). Epub 2021 Jul 13.

Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia (Central University), New Delhi 110025, India.

A label free electrochemical sensor based on pure titanium oxide and manganese (Mn)-doped titanium oxide (TiO) nanoparticles are fabricated and characterized for the sensitive detection of myoglobin (Mb) levels to analyze the cardiovascular infarction. Pristine and Mn-doped TiO nanoparticles were synthesized via the sol-gel method and characterized in order to understand their structure, morphologies, composition and optical properties. The structural properties revealed that the pure- and doped-TiO nanoparticles possess different TiO planes. Read More

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Riminophenazine Derivatives as Potential Antituberculosis Agents: Synthesis, Biological, and Electrochemical Evaluations.

Molecules 2021 Jul 10;26(14). Epub 2021 Jul 10.

Division of Molecular Biology and Human Genetics, Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Stellenbosch University, Tygerberg 7505, South Africa.

A series of novel riminophenazine derivatives, having ionizable alkyl substituents at N-5 and a variety of substituents on the C-3 imino nitrogen, at C-8 and on the pendant aryl group, have been designed and synthesized. Preliminary investigations into the relationship between lipophilicity, redox potential, and antimycobacterial activity were conducted, using the in vitro activity against HRv, mammalian cytotoxicity, and the redox potential of the compounds determined by cyclic voltammetry as measures. Results revealed an activity "cliff" associated with C-8 substitution ( and ) that, along with defined redox activity, point to a new class of riminophenazines as potential anti-tuberculosis agents having reasonable activity (MIC ~1 µM). Read More

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Structure-Activity Relationships of the Antimalarial Agent Artemisinin 10. Synthesis and Antimalarial Activity of Enantiomers of -5β-Hydroxy-d-Secoartemisinin and Analogs: Implications Regarding the Mechanism of Action.

Molecules 2021 Jul 8;26(14). Epub 2021 Jul 8.

Department of BioMolecular Sciences, Division Medicinal Chemistry, School of Pharmacy, University of Mississippi, University, MS 38677, USA.

An efficient synthesis of -6-desmethyl-5β-hydroxy-d-secoartemisinin , a tricyclic analog of -(+)-artemisinin , was accomplished and the racemate was resolved into the (+)- and (-)- enantiomers via their Mosher Ester diastereomers. Antimalarial activity resided with only the artemisinin-like enantiomer -(-)-. Several new compounds -, , , and were synthesized from - but the C-5 secondary hydroxyl group was surprisingly unreactive. Read More

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Monochelic Versus Telechelic Poly(Methyl Methacrylate) as a Matrix for Photoluminescent Nanocomposites with Quantum Dots.

Molecules 2021 Jul 7;26(14). Epub 2021 Jul 7.

Faculty of Chemistry, M.V. Lomonosov Moscow State University, Leninskie Gory 1-3, 119991 Moscow, Russia.

Nanocomposites based on CdSe or CdSe/ZnS quantum dots (QDs) and poly(methyl methacrylate) (PMMA) of different molecular weights and functionality were synthesized by ligand exchange of oleic acid with RAFT-based PMMA. The successful ligand exchange was confirmed by dynamic light scattering in combination with the approach "macromolecules-ghosts" and transmission electron microscopy. Comparative study of mono- and telechelics of PMMA revealed the similarities and differences in their behavior in formation of complexes with QDs and the optical properties of the corresponding nanocomposites. Read More

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Green TPUs from Prepolymer Mixtures Designed by Controlling the Chemical Structure of Flexible Segments.

Int J Mol Sci 2021 Jul 12;22(14). Epub 2021 Jul 12.

Department of Polymer Technology, Faculty of Chemistry, Gdansk University of Technology, 11/12 Gabriela Narutowicza Street, 80-233 Gdansk, Poland.

This study concerns green thermoplastic polyurethanes (TPU) obtained by controlling the chemical structure of flexible segments. Two types of bio-based polyether polyols-poly(trimethylene glycol)s-with average molecular weights ca. 1000 and 2700 Da were used (PO3G1000 and PO3G2700, respectively). Read More

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GhKWL1 Upregulates but Its Function Is Impaired by Binding with VdISC1, a Pathogenic Effector of .

Int J Mol Sci 2021 Jul 8;22(14). Epub 2021 Jul 8.

Biotechnology Research Center, Southwest University, No. 2 Tiansheng Road, Beibei, Chongqing 400716, China.

Verticillium wilt, caused by , is a devastating disease for many important crops, including cotton. Kiwellins (KWLs), a group of cysteine-rich proteins synthesized in many plants, have been shown to be involved in response to various phytopathogens. To evaluate genes for their function in resistance to Verticillium wilt, we investigated KWL homologs in cotton. Read More

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Synthesis of Graphene Oxide from Agave Fiber Tequilana Weber by Hydrothermal Method.

Nanotechnology 2021 Jul 23. Epub 2021 Jul 23.

Universidad Michoacana de San Nicolas de Hidalgo, Francisco J, Mujica SN. Felicitas del Río, Morelia, Michoacán, Morelia, Michoacán, 58060, MEXICO.

Lignocellulosic residues are an important biomass source in Mexico, which can be considered as starting materials for obtaining carbon materials. In this work, carbon materials were produced by pyrolysis of Agave Fiber. The results obtained revealed that the hydrothermal process was successfully used for the synthesis of carbon fibers and subsequently potentiate the production of graphite sheets and graphene oxide (GO), after determining and optimizing the reaction conditions. Read More

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α-d-Mannoside ligands with a valency ranging from one to three: Synthesis and hemagglutination inhibitory properties.

Carbohydr Res 2021 Jul 8;508:108396. Epub 2021 Jul 8.

Department of Chemistry, Jordan University of Science and Technology, PO Box 3030, Irbid 22110, Jordan.

Six mono-, di-, and trivalent α-d-mannopyranosyl conjugates built on aromatic scaffolds were synthesized in excellent yields by Cu(I) catalyzed azide-alkyne cycloaddition reaction (CuAAC). These conjugates were designed to have unique, flexible tails that combine a mid-tail triazole ring, to interact with the tyrosine gate, with a terminal phenyl group armed with benzylic hydroxyl groups to avoid solubility problems as well as to provide options to connect to other supports. Biological evaluation of the prepared conjugates in hemagglutination inhibition (HAI) assay revealed that potency increases with valency and the trivalent ligand 6d (HAI = 0. Read More

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