Design, synthesis and preliminary bioactivity studies of 2-thioxo-4-thiazolidinone derivatives as Bcl-2 inhibitors

被引：30

作者：

Wan, Yichao ^{[1
]}

Wu, Shaolei ^{[1
]}

Xiao, Guizhi ^{[1
]}

Liu, Tingting ^{[1
]}

Hou, Xuben ^{[1
]}

Chen, Chen ^{[1
]}

Guan, Peng ^{[1
]}

Yang, Xinying ^{[1
]}

Fang, Hao ^{[1
]}

机构：

[1] Shandong Univ, Sch Pharm, Dept Med Chem, Key Lab Chem Biol,Minist Educ, Jinan 250012, Shandong, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2015年 / 23卷 / 09期

关键词：

Bcl-2; 2-Thioxo-4-thiazolidinone; Anti-tumor; Inhibitors; SMALL-MOLECULE INHIBITORS; CELL; APOPTOSIS; PROTEINS; CANCER; DISCOVERY; COMPOUND; PATHWAYS; DOMAIN; AGENTS;

D O I：

10.1016/j.bmc.2015.03.024

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：

The B-cell lymphoma-2 (Bcl-2) protein is a promising target for cancer therapy. In the present study, a series of 2-thioxo-4-thiazolidinone derivatives were designed and synthesized as Bcl-2 inhibitors. Most of them possessed decent inhibitory activity for anti-apoptotic Bcl-2 proteins. Among them, compound 31 has similar growth inhibition towards K562 compared to (R)-Gossypol. In addition, it inhibits the myeloid cell leukemia sequence 1 (Mcl-1) protein with a K-i value of 74 nM. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：1994 / 2003

页数：10

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