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Design, synthesis and pharmacological evaluation of new acyl sulfonamides as potent and selective Bcl-2 inhibitors 期刊论文

编号：

60c66ec4-4c6c-4bc2-b7c4-0f367f88fc79
作者：

Liu, Xiaohua^[1,2];Zhang, Yu(张瑜)^[3]Huang, Wenjing^[3];Tan, Wenfu(谭文福)^[3]Zhang, Ao^[1,2,4];
语种：

English
期刊：

BIOORGANIC & MEDICINAL CHEMISTRY ISSN：0968-0896 2018 年 26 卷 2 期 (443 - 454) ; JAN 15
收录：
关键词：

Bcl-2 Bcl-xL Sulfonamide Navitoclax Apoptosis
摘要：

The antiapoptotic protein Bcl-2, overexpressed in many tumor cells, is an attractive target for potential small molecule anticancer drug discovery. Herein, we report a different structural modification approach on ABT-263 by merging the piperazinyl-phenyl fragment into a bicyclic framework leading to a series of novel analogues, among which tetrahydroisoquinoline 13 was nearly equally potent against Bcl-2 as ABT-263. Further SAR in the P4-interaction pocket affored the difluoroazetidine substituted analogue 55, which retained good Bcl-2 activity with improved Bcl-2/Bcl-xL selectivity. (C) 2017 Elsevier Ltd. All rights reserved.
推荐引用方式
GB/T 7714：

Liu Xiaohua,Zhang Yu,Huang Wenjing, et al. Design, synthesis and pharmacological evaluation of new acyl sulfonamides as potent and selective Bcl-2 inhibitors [J].BIOORGANIC & MEDICINAL CHEMISTRY,2018,26(2):443-454.
APA：

Liu Xiaohua,Zhang Yu,Huang Wenjing,Tan Wenfu,&Zhang Ao.(2018).Design, synthesis and pharmacological evaluation of new acyl sulfonamides as potent and selective Bcl-2 inhibitors .BIOORGANIC & MEDICINAL CHEMISTRY,26(2):443-454.
MLA：

Liu Xiaohua, et al. "Design, synthesis and pharmacological evaluation of new acyl sulfonamides as potent and selective Bcl-2 inhibitors" .BIOORGANIC & MEDICINAL CHEMISTRY 26,2(2018):443-454.

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