Synthesis of the analogs of plocabulin and their preliminary structure-activity relationship study
文献类型：期刊论文
| 作者 | Wang, Leiming1,2; Li, Xin3; Cui, Hong2; Lei, Xinsheng2; Liu, Hongchun3 ; Wang, Quanrui1; Li, Yingxia2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2021-11-01 |
| 卷号 | 51页码:5 |
| 关键词 | Marine nature products Plocabulin PM060184 Synthesis Antiproliferation |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2021.128355 |
| 通讯作者 | Liu, Hongchun(hchliu@simm.ac.cn) ; Wang, Quanrui(qrwang@fudan.edu.cn) ; Li, Yingxia(liyx417@fudan.edu.cn) |
| 英文摘要 | Plocabulin, a marine natural polyketide isolated from the sponge Lithoplocamia lithistoides, is a novel and potent microtubule-destabilizing agent. Guided by the reported binding mode, several new analogs of plocabulin have been designed through removing the right aliphatic chain and further modifying on the carbamate group and the enamide unit. The preliminary results indicate that the right aliphatic chain in plocabulin is allowed to remove with a little loss of activity, the carbamate group plays a role in the activity, and particularly, the enamide unit has an important effect on the activity. This new finding will aid the design of novel potent tubulin-binding agents based on plocabulin. |
| WOS关键词 | POTENT ANTITUMOR-ACTIVITY ; INHIBITORS |
| 资助项目 | National Natural Science Foundation of China[81773576] ; National Key R&D Program of China[2018YFC0310905] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000709694400003 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/298341]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Liu, Hongchun; Wang, Quanrui; Li, Yingxia |
| 作者单位 | 1.Fudan Univ, Dept Chem, 2005 Songhu Rd, Shanghai 200438, Peoples R China 2.Fudan Univ, Sch Pharm, Dept Med Chem, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Leiming,Li, Xin,Cui, Hong,et al. Synthesis of the analogs of plocabulin and their preliminary structure-activity relationship study[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2021,51:5. |
| APA | Wang, Leiming.,Li, Xin.,Cui, Hong.,Lei, Xinsheng.,Liu, Hongchun.,...&Li, Yingxia.(2021).Synthesis of the analogs of plocabulin and their preliminary structure-activity relationship study.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,51,5. |
| MLA | Wang, Leiming,et al."Synthesis of the analogs of plocabulin and their preliminary structure-activity relationship study".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 51(2021):5. |
入库方式： OAI收割
来源：上海药物研究所
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