拮抗Mcl-1/Bcl-2的吗啉代-1H-菲衍生物的设计、合成及构效关系研究
Design, synthesis and structure–activity relationship studies of morpholino-1H-phenalene derivatives that antagonize Mcl-1/Bcl-2.
作者信息
Li Xiangqian, Liang Xiaomeng, Song Ting, Su Pengchen, Zhang Zhichao
机构信息
State Key Laboratory of Fine Chemicals, School of Chemistry, Dalian University of Technology, Dalian, China.
出版信息
Bioorg Med Chem. 2014 Nov 1;22(21):5738-46. doi: 10.1016/j.bmc.2014.09.047. Epub 2014 Oct 2.
PMID:25584387
Abstract
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.
摘要
我们在此报告Mcl-1和Bcl-2双重抑制剂的特性研究。研究发现，与占据p2口袋的疏水基团相比，与R263形成氢键的突出羰基起主要作用。设计、合成并评估了一系列代表吗啉代-1H-菲不同部分的双重抑制剂。
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