Synthesis of the analogs of plocabulin and their preliminary structure-activity relationship study

doi:10.1016/j.bmcl.2021.128355

	Synthesis of the analogs of plocabulin and their preliminary structure-activity relationship study
	Wang, Leiming 1,2; Li, Xin 3; Cui, Hong 2; Lei, Xinsheng 2; Liu, Hongchun 3; Wang, Quanrui 1; Li, Yingxia 2
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	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.
资助项目	National Natural Science Foundation of China[81773576] ; National Key R&D Program of China[2018YFC0310905]
WOS关键词	POTENT ANTITUMOR-ACTIVITY ; INHIBITORS
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000709694400003
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/298341]
专题	中国科学院上海药物研究所
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.