Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma

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成果类型：

期刊论文

作者：

Zhou, Ruolan;Fan, Shaoyu;Zhang, Minmin;Zhang, Qingsen;Hu, Jian;...

通讯作者：

Chen, Xin;Zheng, Canhui;Shen, Aijun

作者机构：

[Chen, Xin; Zhou, Ruolan; Fan, Shaoyu] Wuhan Polytech Univ, Sch Biol & Pharmaceut Engn, Wuhan 430023, Hubei, Peoples R China.

[Hu, Jian; Wang, Mingping; Wang, Chongqing; Zheng, Canhui; Zhu, Ju; Zhang, Qingsen; Zhou, Ruolan; Fan, Shaoyu] Second Mil Med Univ, Sch Pharm, Shanghai 200433, Peoples R China.

[Zhang, Minmin; Shen, Aijun] Chinese Acad Sci, SIMM, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China.

通讯机构：

[Chen, Xin] W

[Zheng, Canhui] S

[Shen, Aijun] C

Wuhan Polytech Univ, Sch Biol & Pharmaceut Engn, Wuhan 430023, Hubei, Peoples R China.

Second Mil Med Univ, Sch Pharm, Shanghai 200433, Peoples R China.

语种：

英文

关键词：

Anti-tumor agents;Bcl-2 inhibitors;Dualtarget inhibitors;HDAC inhibitors;HDAC6 inhibitors;Multiple myeloma

期刊：

Bioorganic & Medicinal Chemistry Letters

ISSN：

0960-894X

年：

2019

卷：

期：

页码：

349-352

DOI：

10.1016/j.bmcl.2018.12.052

基金类别：

We thank the Shanghai Rising-Star Program of China ( 16QA1404800 ), the State Key laboratory of Drug Research of China ( SIMM1601KF-01 ), and the National Natural Science Foundation of China (Grant Nos. 21572266 and 81673472 ) for financial support.

机构署名：

本校为第一且通讯机构

院系归属：

生命科学与技术学院

摘要：

Multiple myeloma (MM) is the second most common haematological malignancy. Almost all patients with MM eventually relapse, and most recommended treatment protocols for the patients with relapsed refractory MM comprise a combination of drugs with different mechanisms of action. Therefore novel drugs are in urgent need in clinic. Bcl-2 inhibitors and HDAC inhibitors were proved their anti-MM effect in clinic or under clinical trials, and they were further discovered to have synergistic interactions. In this study, a series of Bcl-2/HDAC dual-target inhibitors were designed and synthesized. Among...

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Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma

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