Design, synthesis and structure-activity relationship studies of morpholino-1H-phenalene derivatives that antagonize Mcl-1/Bcl-2

被引：8

作者：

Li, Xiangqian ^{[1
,2
]}

Liang, Xiaomeng ^{[1
]}

Song, Ting ^{[1
]}

Su, Pengchen ^{[1
]}

Zhang, Zhichao ^{[1
]}

机构：

[1] Dalian Univ Technol, Sch Chem, State Key Lab Fine Chem, Dalian, Peoples R China

[2] Ocean Univ China, Qingdao, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2014年 / 22卷 / 21期

基金：

中国国家自然科学基金;

关键词：

Dual inhibitors; Hydrogen bond; Apoptosis; Mcl-1; Bcl-2; SMALL-MOLECULE INHIBITORS; BCL-2; FAMILY; MCL-1; APOPTOSIS; PROTEIN; DISCOVERY; BCL-X(L);

D O I：

10.1016/j.bmc.2014.09.047

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We report herein characteristic studies of Mcl-1 and Bcl-2 dual inhibitors. It was found that a protruding carbonyl group forming hydrogen bond with R263 plays a predominant role compared with the hydrophobic group that occupies the p2 pocket. A series of dual inhibitors representing different parts of the morpholino-1H-phenalene were designed, synthesized and evaluated. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：5738 / 5746

页数：9

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