Design and synthesis of novel PEG-conjugated 20(S)-camptothecin sulfonylamidine derivatives with potent in vitro antitumor activity via Cu-catalyzed three-component reaction

doi:10.1016/j.bmcl.2015.04.060

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	Design and synthesis of novel PEG-conjugated 20(S)-camptothecin sulfonylamidine derivatives with potent in vitro antitumor activity via Cu-catalyzed three-component reaction
	Song, ZL; Chen, HL; Wang, YH; Goto, M; Gao, WJ; Cheng, PL; Morris-Natschke, SL; Liu, YQ; Zhu, GX; Wang, MJ
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2015-07-01
卷号	25 期号:13 页码:2690-2693
关键词	Camptothecin C-20 position Cytotoxic activity Poly(ethylene glycol) (PEG) Sulfonylamidine
ISSN号	0960-894X
DOI	10.1016/j.bmcl.2015.04.060
文献子类	Article
英文摘要	In our continuing search for camptothecin (CPT)-derived antitumor drugs, novel structurally diverse PEG-based 20(S)-CPT sulfonylamidine derivatives were designed, synthesized via a Cu-multicomponent reaction (MCR), and evaluated for cytotoxicity against four human tumor cell lines (A-549, MDA-MB-231, KB, and KBvin). All of the derivatives showed promising in vitro cytotoxic activity against the tested tumor cell lines, and were more potent than irinotecan. Significantly, these derivatives exhibited comparable cytotoxicity against KBvin, while irinotecan was less active against this cell line. With a concise efficient synthesis and potent cytotoxic profiles, especially significant activity towards KBvin, these compounds merit further development as a new generation of CPT-derived PEG-conjugated drug candidates. (C) 2015 Elsevier Ltd. All rights reserved.
学科主题	Pharmacology & Pharmacy ; Chemistry
出版地	OXFORD
资助项目	国家自然科学基金项目 ; 中央高校基本科研业务费专项资金 ; 美国国立卫生研究院项目
项目编号	National Natural Science Foundation of China [30800720, 31371975] ; Fundamental Research Funds for the Central Universities [lzujbky-2014-k19] ; NIH Grant from the National Cancer Institute [CA177584] ; Health and Welfare Surcharge of Tobacco Products, China Medical University Hospital Cancer Research Center of Excellence, Taiwan [MOHW103-TD-B-111-03]
语种	英语
WOS记录号	WOS:000355343300018
资助机构	NSFC ; LZU ; NIH
内容类型	期刊论文
源URL	[http://ir.lzu.edu.cn/handle/262010/179552]
专题	药学院_期刊论文
通讯作者	Liu, YQ (reprint author), Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China.
推荐引用方式 GB/T 7714	Song, ZL,Chen, HL,Wang, YH,et al. Design and synthesis of novel PEG-conjugated 20(S)-camptothecin sulfonylamidine derivatives with potent in vitro antitumor activity via Cu-catalyzed three-component reaction[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2015,25(13):2690-2693.
APA	Song, ZL.,Chen, HL.,Wang, YH.,Goto, M.,Gao, WJ.,...&Liu, YQ .(2015).Design and synthesis of novel PEG-conjugated 20(S)-camptothecin sulfonylamidine derivatives with potent in vitro antitumor activity via Cu-catalyzed three-component reaction.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,25(13),2690-2693.
MLA	Song, ZL,et al."Design and synthesis of novel PEG-conjugated 20(S)-camptothecin sulfonylamidine derivatives with potent in vitro antitumor activity via Cu-catalyzed three-component reaction".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 25.13(2015):2690-2693.