Design, Synthesis, Biological Evaluation, and Molecular Docking Studies of Indazole Derivatives as Bcl-2/Mcl-1 Dual Inhibitors

被引：3

作者：

Luo, Xi ^{[1
]}

Deng, Xu ^{[1
]}

Ruan, Jingyi ^{[1
]}

Wang, Wenyan ^{[1
]}

Wan, Yichao ^{[1
,2
]}

机构：

[1] Hunan Univ Sci & Technol, Sch Chem & Chem Engn, Key Lab Theoret Organ Chem & Funct Mol, Minist Educ, Xiangtan 411201, Hunan, Peoples R China

[2] Hunan Univ Sci & Technol, Hunan Prov Key Lab Controllable Preparat & Funct, Hunan Prov Key Lab Adv Mat New Energy Storage & C, Xiangtan 411201, Hunan, Peoples R China

来源：

RUSSIAN JOURNAL OF GENERAL CHEMISTRY | 2022年 / 92卷 / 06期

基金：

中国国家自然科学基金;

关键词：

Bcl-2; Mcl-1 dual inhibitors; indazole derivatives; anti-tumor; scaffold hopping;

D O I：

10.1134/S1070363222060238

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

In this study, a series of new indazole derivatives has been designed, synthesized and evaluated for inhibitory activity against anti-apoptotic Bcl-2 proteins (Bcl-2, Mcl-1, Bcl-xL). Among them, three products have demonstrated high inhibitory activity against Bcl-2/Mcl-1, which is similar to that of the positive control compound WL-276. Their poor Bcl-xL inhibitory activity allows to avoid platelet toxicity caused by Bcl-xL inhibition. Hence, they might be considered as lead compounds for developing Bcl-2/Mcl-1 dual inhibitors of higher potency.

引用

页码：1109 / 1114

页数：6

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