Design,synthesis,evaluation and 3D-QSAR analysis of benzosulfonamide benzenesulfonates as potent and

来源 :第八届国际分子模拟与信息技术应用学术会议 | 被引量 : 0次 | 上传用户：gswwg

【摘要】

：

　　A novel series of MMPIs was designed,synthesized and purified using a scaffold modification strategy.The new compounds were also evaluated for biological ac

【作者】

：

Han-YueQiu;Zhong-ChangWang;Peng-FeiWang;Xiao-QiangYan;Xiao-MingWang;Yong-HuaYang;Hai-LiangZhu;

【机构】

：

State Key Laboratory of Pharmaceutical Biotechnology,Nanjing University,Nanjing 210093,pevple's Rep

【出处】

：

第八届国际分子模拟与信息技术应用学术会议

【发表日期】

：

2016年期

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　　A novel series of MMPIs was designed,synthesized and purified using a scaffold modification strategy.The new compounds were also evaluated for biological activity against A549.MCF-7.HepG2 and Hela as potential inhibitors of MMP-2 The most potent inhibitor against MMP-2 was compound 19(IC50=0.38 μM).Its antitumor effect is believed to be due to the induction of apoptosis.which is further confirmed by Annexin V-FITC/PI staining assay using flow cytometry analysis.Furthermore,all the compounds were evaluated for cytotoxicity against 293T.In addition,3D-QSAR studies were conducted.The result showed that the benzosulfonamide benzenesulfonate MMPIs may prove interesting lead candidates to target MMP-2 associated tumor,where the MMP-2 domain is located extracellularly.

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Design,synthesis,evaluation and 3D-QSAR analysis of benzosulfonamide benzenesulfonates as potent and

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