Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma
文献类型：期刊论文
| 作者 | Zhou, Ruolan1,2; Fang, Shaoyu1,2; Zhang, Minmin3 ; Zhang, Qingsen4; Hu, Jian4; Wang, Mingping4; Wang, Chongqing4; Zhu, Ju4; Shen, Aijun3; Chen, Xin1
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| 刊名 | Bioorganic & medicinal chemistry letters
 |
| 出版日期 | 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 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/266313]  |
| 专题 | 新药研究国家重点实验室 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). |
入库方式： OAI收割
来源：上海药物研究所
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