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

doi:10.1016/j.bmcl.2018.12.052

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药理学第一研究室

	Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma
	Zhou, Ruolan 1,2; Fang, Shaoyu 1,2; Zhang, Minmin3 ; Zhang, Qingsen 4; Hu, Jian 4; Wang, Mingping 4; Wang, Chongqing 4; Zhu, Ju 4; Shen, Aijun3 ; Chen, Xin 1
刊名	Bioorganic & medicinal chemistry letters
	2018-12-22
ISSN号	1464-3405
DOI	10.1016/j.bmcl.2018.12.052
文献子类	Article
英文摘要	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 them, compounds 7e-7g showed good inhibitory activities against HDAC6 and high binding affinities to Bcl-2 protein simultaneously. They also displayed good growth inhibitory activities against human MM cell line RPMI-8226, which proved their potential value for the treatment of multiple myeloma.
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/266313]
专题	药理学第一研究室
通讯作者	Shen, Aijun; Chen, Xin; Zheng, Canhui
作者单位	1.School of Biology and Pharmaceutical Engineering, Wuhan Polytechnic University, Wuhan 430023, China; 2.School of Pharmacy, Second Military Medical University, Shanghai 200433, China; 3.Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China; 4.School of Pharmacy, Second Military Medical University, Shanghai 200433, China
推荐引用方式 GB/T 7714	Zhou, Ruolan,Fang, Shaoyu,Zhang, Minmin,et al. Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma[J]. Bioorganic & medicinal chemistry letters,2018.
APA	Zhou, Ruolan.,Fang, Shaoyu.,Zhang, Minmin.,Zhang, Qingsen.,Hu, Jian.,...&Zheng, Canhui.(2018).Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma.Bioorganic & medicinal chemistry letters.
MLA	Zhou, Ruolan,et al."Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma".Bioorganic & medicinal chemistry letters (2018).