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Chinese Journal of Structural Chemistry 2020年第6期39卷 1157-1166页

作者： SHI Jian-Cheng HUANG Xiao-Qian LUO Min HUANG Chu-Sheng College of Chemistry and Material Nanning Normal UniversiyNanning 530001China

The three-dimensional quantitative structure-activity relationships(3D-QSAR)for 37 curcumin derivatives were constructed by CoMFA and CoMSIA methods,*** results showed that the cross validated coefficient(q^2)and non-cross-validated coefficient(R^2)were 0.711,0.962 in CoMFA model and 0.774,0.856 in CoMSIA model,respectively,which suggests that two models are robust and have good exterior predictive *** on these two models and the binding mode with tubulin,nine novel curcuminoids inhibitors which could exhibit much higher anticancer potency and efficiently occupy the colchicine binding site of tubulin,were *** expect that the results in this paper have the potential to facilitate the process of design and to develop new potent curcumin derivatives with stronger anticancer activities.

关键词： anticancer activity tubulin curcumin derivatives 3D-QSAR molecular docking molecular design

Design, Synthesis and Biological Activities of N-（Furan-2-ylmethyl）-lH-indole-3-carboxamide Derivatives as Epidemal Growth Factor Receptor Inhibitors and anticancer Agents

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Chemical Research in Chinese Universities 2017年第3期33卷 365-372页

作者： ZHANG Lan DENG Xinshan WU Jiaofeng MENG Guangpeng LIU Congchong CHEN Guzhou ZHAO Qingchun HU Chun Key Laboratory of Structure-based Drug Design & Discovery Ministry of Education Shenyang Pharmaceutical University Shenyang 110016 P. R. China Department of Pharmacy General Hospital of Shenyang Military Area Command Shenyang 110016 P. R. China

A series ofN-（furan-2-ylmethyl）-lH-indole-3-carboxamide derivatives（6a--6p） was designed and synthe- sized for developing novel indole scaffolds as anticancer agents targeting the epidemal growth factor receptor （EGFR）, and the cytotoxic activities of the target compounds were evaluated against three EGFR high-expressed cancer cell lines[human lung adenocarcinoma cell line（A549）, Henrietta Lacks strain of cancer cell line（HeLa） and human colorectal cancer cell line（SW480）], one EGFR low-expressed cell line（human liver cancer cell line, HepG2） and one human liver normal cell line（HL7702） using 3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyl tetrazolium bromide （MTT） assay, Some target compounds exhibited potent anficancer activities against A549, HeLa, SW480 and weak activities on HepG2, which signifies that the target compounds are likely to be EGFR inhibitors as expected. And they showed weak cytotoxic effects on HL7702, which implies the target compounds are probably to be of low toxicity against normal cells. Among them, the target compound 1-ethyl-N-（fttran-2-ylmethyl）-5-{2-{ [2-（2-methoxy- phenoxy）ethyl]amino}-2-oxoethoxy}-2-methyl-1H-indole-3-carboxamide（6p） with 2-{[2-（2-methoxyphenoxy）ethyl]- amino}-2-oxoethoxy group at the C5 position of the N-（furan-2-ylmethyl）-lH-indole-3-carboxamide scaffold exhibited the most potent anticancer activity. Also the binding interaction of the target compound 6p with EGFR was explored by molecular docking. Conclusively, the novel indole scaffold may be beneficial to investigate new anticancer agents for targeting the EGFR.

关键词： anticancer activity Epidemal growth factor receptor(EGFR) inhibitor N-(Furan-2-ylmethyl)-lH-indole-3-carboxamide derivative

Synthesis, Biological Evaluation and Molecular Docking of Novel Phenylpyrimidine Derivatives as Potential anticancer Agents

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Chemical Research in Chinese Universities 2018年第6期34卷 912-917页

作者： J1N Bo TAO Ye YANG Hongliang Department of Veterinary Medicine North eastAgricultural University Harbin 150030 P. R. China Heilongfiang Key Laboratory for Animal Disease Control and Pharmaceutical Development Harbin 150030 P. R. China School of Pharmaceutical Sciences Jilin University Changchun 130021 P. R. China

Based on our previous researches, a novel phenylpyrimidine pharmacophore model was proposed and fifteen derivatives were synthesized and characterized by means of spectroscopy methods. The inhibitory effects of them were screened against HeLa cell line by virtue of MTT assay in vitro. The results indicate some of the phenyl- pyrimidine derivatives exhibit potent biological activities. Among them, compounds 6g and 6h exhibit the best activity at half maximal inhibitory concentrations of 1.5 and 2.8 μmol/L, respectively. These compotmds also exhibit good activities against HepG2 cell line and MCF-7 cell line. FLT-3 kinase was screened as the most potent molecular target. Computational docking between compound 6g and FLT-3 was carried ont to interpret the binding mode. The results show phenylpyrimidine derivatives have effective antitumor activities, which provides a base for further research of them as antitumor agents.

关键词： Phenylpyrimidine anticancer activity Molecular docking

Potato protease inhibitors,a functional food material with antioxidant and anticancer potential

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Food Science and Human Wellness 2023年第5期12卷 1762-1771页

作者： Yaotong Liu Yuanyuan Bian Yan Bai Siqi Yu Yuxuan Tian Jie Li Suhong Li Tuoping Li College of Food Science Shenyang Agricultural UniversityShenyang 110866China College of Grain Science and Technology Shenyang Normal UniversityShenyang 110034China College of Pharmaceutical Science Liaoning UniversityShenyang 110036China

Potato protease inhibitors(PPIs),as the main component of potato protein isolate,have good safety,nutrition and great market *** antioxidant and anticancer properties of PPIs were evaluated with cellbased biological *** results showed that when the concentration of PPIs was 5 mg/mL,the peroxyl radical scavenging value was(2119±204)mg VCE/100 g,and the cellular antioxidant activity values were(45.83±3.5)(no PBS wash)and(33.25±4.4)μmol QE/100 g(PBS wash).Cells pretreated with PPIs could significantly prevent the oxidative damage induced by H_(2)O_(2),inhibit the morphological changes of cells and maintain the ***,PPIs had selective anti-proliferative effects on GIST882 cells(IC50=(10.53±3.87)mg/mL)and demonstrated potent inhibition of the growth,migration and invasion of cancer *** findings provide a scientific basis for PPIs as promising candidates for functional foods to aid in the prevention of oxidative damage and cancer.

关键词： Potato protease inhibitors Antioxidant activity Cytoprotection anticancer activity

Synthesis of (2R,3aR,8aR)-6-Chloro-3a-hydroxy-1,2,3,3a,8,8a- hexahydropyrrolo[2,3-b]indole-2-carboxylic Acid Methyl Ester by Reductive Cyclization

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Chinese Journal of Chemistry 2004年第4期22卷 365-370页

作者：洪文旭姚祝军 State Key Laboratory of Bioorganic and Natural Products Chemistry Shanghai Institute of Organic Chemistry Chinese Academy of Sciences

A synthesis of (2R,3aR,8aR)-6-chloro-3a-hydroxy-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indole-2-carboxylic acid methyl ester (1) was achieved. An aldol reaction with Garner aldehyde, a hydroxyl introduction by Davis re-agent, and a reductive intramolecular ring-closure reaction were served as the key steps. This piece of work pro-vides a new way to synthesize the analogues of hexahydropyrrolo[2,3-b]indole, starting from readily available chemical substrates and inexpensive reagents.

关键词： aldol reaction Davis oxidation reductive ring-closure reaction indole derivative anticancer activity

Design,Synthesis and Bioactivities Evaluation of Novel Quinazoline Analogs Containing Oxazole Units

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Chinese Journal of Chemistry 2014年第6期32卷 538-544页

作者： Xuehui Hou Jingyu Zhang Xuan Zhao Liming Chang Ping Hu Hongmin Liu Department of Quality Detection and Management Henan University of Animal Husbandry and EconomyZhengzhouHenan 450011China School of Pharmaceutical Science Henan University of TCMZhengzhouHenan 450008China School of Pharmaceutical Science Zhengzhou UniversityZhengzhouHenan 450001China

A novel type of quinazoline derivatives,which were designed by the combination of quinazoline as the back-bone and oxazole scaffold as the substituent,have been synthesized and their biological activities were evaluated for anti-proliferative activities and EGFR inhibitory *** 12b demonstrated the most potent inhibi-tory activity(IC_(50)=0.95μmol/L for EGFR),which could be optimized as a potential EGFR inhibitor in the further *** structures of the synthesized quinazoline analogs and all intermediates were comfirmed by 1H and 13C NMR,2D NMR spectra,IR spectra and MS spectra.

关键词： quinazoline synthesis anticancer activity

Antimicrobial, anticancer and DNA binding studies of transition metal(Ⅱ)complexes containing 2-phenyl-4-selenazole carboxylic acid

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Science China Chemistry 2013年第5期56卷 588-594页

作者： GUAN QuanYin SHI Xia SHEN JinBei ZHAO GuoLiang College of Chemistry and Life Sciences Zhejiang Normal University Zhejiang Normal University Xingzhi College

Three novel transition metal complexes [ML2（phen）]＇H20 （M= Mn, Co, Zn; HL= C10H702NSe, 2-phenyl-4-selenazole carboxylic acid, phen= 1,10-phenanthroline） 1-3 were synthesized and characterized by elemental analysis, IR spectra. Their crystal structures were deterimined by single-crystal X-ray diffraction method. The antibacterial activities of the complexes against five species of bacteria, Escherichia coli （E. coli）, Staphylococcus epidermidis （S. epidermidis）, Staphylococcus aureus （S. au- reus）, Acinetobacter baumanii （A. baumanii） and Streptococcus viridans （S. viridans）, were tested respectively. The anticancer activities of the complexes against human pancreatic cancer line PANC-28 and human hepatocarcinoma line HuH7 were also studied. The interactions between the complexes and DNA were studied by ethidium bromide （EB） fluorescent probe.

关键词： 2-phenyl-4-selenazole carboxylic acid transition metal complex antibacterial activity anticancer activity DNA binding

The phytochemical, biological, and medicinal attributes of phytoecdysteroids: An updated review

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Acta Pharmaceutica Sinica B 2021年第7期11卷 1740-1766页

作者： Niranjan Das Siddhartha Kumar Mishra Anusha Bishayee Eunüs S.Ali Anupam Bishayee Department of Chemistry Iswar Chandra Vidyasagar CollegeBelonia-799155TripuraIndia Cancer Biology Laboratory Department of ZoologySchool of Biological SciencesDr.Harisingh Gour Central UniversitySagar-470003Madhya PradeshIndia Pine View School OspreyFL 34229USA Department of Biochemistry and Molecular Genetics Feinberg School of MedicineNorthwestern UniversityChicagoIL 60611USA Lake Erie College of Osteopathic Medicine BradentonFL 34211USA

The phytoecdysteroids(PEs)comprise a large group of biologically-active plant steroids,which have structures similar to those of insect-molting *** are distributed in plants as secondary metabolites that offer protection against phytophagus(plant-eating)*** insects consume the plants containing these chemicals,they promptly molt and undergo metabolic destruction;the insects eventually ***,ecdysteroids are a group of polyhydroxylated ketosteroids that are structurally similar to *** carbon skeleton of ecdysteroids is termed as cyclopentanoperhydro-phenanthrene with aβ-side chain at *** essential characteristics of ecdysteroids are a cis-(5β-H)junction of rings A and B,a 7-en-6-one chromophore,and a trans(14α-OH)junction of rings C and *** only synthesize PEs from mevalonic acid in the mevalonate pathway of the plant cell using acetyl-CoA as a precursor;the most common PE is *** far,over 400 PEs have been identified and reported,and a compilation of 166 PEs originating from 1998 has been previously *** the present review,we have summarized 212 new PEs reported between 1999 and *** have also critically analyzed the biological,pharmacological,and medicinal properties of PEs to understand the full impact of these phytoconstituents in health and disease.

关键词： Phytoecdysteroids Secondary metabolites Antioxidant Anti-inflammatory Antimicrobial Antidiabetic anticancer activity

Synthesis, Preliminary Structure-activity Relationships and Biological Evaluation of Pyridinyl-4,5-2H-isoxazole Derivatives as Potent Antitumor Agents

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Chemical Research in Chinese Universities 2017年第1期33卷 61-69页

作者： YANG Hongliang XU Guoxing PEI Yazhong College of Veterinary Medicine Northeast Agricultural University Harbin 150030 P. R. China School of Pharmaceutical Sciences Jilin University Changchun 130021 P. R. China

A series of novel pyridinyl-4,5-2H-isoxazole derivatives was synthesized and their chemical structures were characterized by 1H NMR, 13C NMR as well as MS spectroscopic methods, their melting points were also determined. The inhibitory effects of them against breast cancer cell lme（MCF-7） were evaluated by 3-（4,5-dimethyl- 2-thiazolyl）-2,5-diphenyl-2-H-tetrazolium bromide（MTT） procedure in vitro. Most of them possesed potent anti- proliferative activities, among which compounds llc and llj exhibited half maximal inhibitory concentrations（IC50） of 1.9 and 1.5 μmol/L, respectively. These compounds also exhibited potent anti-proliferative activities against both human hepatoma cell line（HepG2） and cervical cancer cell line（HeLa）. Preliminary structure-activity relationship （SAR） information from these compounds can be used to guide further exploration of new compounds with better potency as molecular probes. Further study on the mechanism-of-action of these compounds is under investigation.

关键词： Pyridine Isoxazole anticancer activity Chemotherapeutic agent

Synthesis, Anti-lung Cancer activity and Docking Study of New Organic Compounds

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Chinese Journal of Structural Chemistry 2020年第6期39卷 1119-1125页

作者： LI Di Inner Mongolia University for Nationalities Tongliao 028000China

Novel organic compounds(1~8) were designed, synthesized and characterized by IR, ~1H NMR, H RMS, and single-crystal X-ray crystallography. The anticancer activities of these compounds were investigated against four human lung cancer cells(H20, H2227, H69 and H524) by 3-(4,5)-dimethylthiahiazo(-z-y1)-3,5-di-phenytetrazoliumromide(MTT) assay. Furthermore, by taking compounds 1 and 5 as representatives, molecular docking studies supported the biological assay data, suggesting that compared with 1, compound 5 has stronger interaction with protein.

关键词： MTT assay anticancer activity molecular docking