Molecular modeling and synthesis of new 1,5-diphenylpyrazoles as breast cancer cell growth inhibitors

Author:

Ewes Wafaa A.1,Badr Sahar M.I.1,Eisa Hassan M.1,Nasr Magda N.A.1

Affiliation:

1. 1Faculty of Pharmacy, Department of Pharmaceutical Organic Chemistry, University of Mansoura, Mansoura 35516, Egypt

Abstract

AbstractNew pyrazoles have been synthesized and evaluated as breast cancer cell growth inhibitors. Condensation of the substituted pyrazole-4-carbaldehyde1with acetophenone and chloroacetophenone afforded α, β-unsaturated ketones2and3, respectively. Compounds2and3were subjected to different reactions using hydrazine hydrate, substituted hydrazine hydrate, hydroxylamine,o-phenylenediamine, malononitrile under different conditions affording 4-substituted pyrazole derivatives4–28. Structure elucidation of these compounds was conducted using IR,1H NMR,13C NMR, mass spectral data and elemental analysis. Antitumor activity of target compounds was tested against MCF-7 cell line (human breast cancer). Compounds4,10and20show significant antitumor activity against breast cancer. Docking was performed with protein 1UYK to study the binding mode of the designed compounds.

Publisher

Walter de Gruyter GmbH

Subject

Organic Chemistry

Reference100 articles.

1. Server a web server for potential drug target identification via pharmacophore mapping approach;Liu;Nucleic Acids Res,2010

2. Synthesis of novel oxime - containing pyrazole derivatives and discovery of regulators for apoptosis and autophagy in lung cancer cells;Zheng;Bioorg Med Chem Lett,2010

3. Solid - phase synthesis and biological evaluation of a parallel library of dihydro benzothiazepines;Ansari;Med Chem,2008

4. Synthesis of novel pyrazolic analogues of chalcones and their aryl aryl dihydro pyrazol yl phenyl pyrazole derivatives as potential antitumor agents;Insuasty;Med Chem,2010

5. a versatile pharmacophore a;Bariwal;review Eur Med Chem,2008

同舟云学术

1.学者识别学者识别

2.学术分析学术分析

3.人才评估人才评估

"同舟云学术"是以全球学者为主线,采集、加工和组织学术论文而形成的新型学术文献查询和分析系统,可以对全球学者进行文献检索和人才价值评估。用户可以通过关注某些学科领域的顶尖人物而持续追踪该领域的学科进展和研究前沿。经过近期的数据扩容,当前同舟云学术共收录了国内外主流学术期刊6万余种,收集的期刊论文及会议论文总量共计约1.5亿篇,并以每天添加12000余篇中外论文的速度递增。我们也可以为用户提供个性化、定制化的学者数据。欢迎来电咨询!咨询电话:010-8811{复制后删除}0370

www.globalauthorid.com

TOP

Copyright © 2019-2024 北京同舟云网络信息技术有限公司
京公网安备11010802033243号  京ICP备18003416号-3