Synthesis and antitumor activity of the hexacyclic camptothecin derivatives

doi:10.1016/j.bmcl.2005.04.063

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	Synthesis and antitumor activity of the hexacyclic camptothecin derivatives
	Gao, HY; Zhang, XW; Chen, Y; Shen, HW; Pang, T; Sun, J; Xu, CH; Ding, J; Li, C; Lu, W
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2005-07-01
卷号	15 期号:13 页码:3233-3236
关键词	camptothecin topoisomerase I antitumor activity
ISSN号	0960-894X
DOI	10.1016/j.bmcl.2005.04.063
文献子类	Article
英文摘要	A series of hexacyclic camptothecin derivatives were synthesized to test for antitumor activity as topoisomerase I inhibitor. The strategy of synthesis was used for the formation of additional furan and dihydrofuran rings fused with 9- and 10-positions of camptothecin. All of the hexacyclic camptothecins were assayed for cytotoxicity against four human tumor cell lines, HL60, BEL-7402, HCT-116, and HeLa, and showed very impressive cytotoxicity activity in vitro. Enzyme activity of the hexacyclic camptothecins was evaluated, being equal or superior to that of SN-38. The stability of four compounds was assessed in human plasma. Two of these compounds were chosen to test for antitumor activity in vivo against Sarcoma-180. The results suggested that additional furan and dihydrofuran rings could improve the antitumor activity in vitro and vivo, though the stability of the lactone ring did not increase. (c) 2005 Elsevier Ltd. All rights reserved.
WOS关键词	DNA-TOPOISOMERASE-I ; ANALOGS ; RING
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000230062300012
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/273840]
专题	药理学第一研究室药物化学研究室
通讯作者	Lu, W
作者单位	Chinese Acad Sci, Shanghai Inst Mat Med, SIBS, Grad Sch, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Gao, HY,Zhang, XW,Chen, Y,et al. Synthesis and antitumor activity of the hexacyclic camptothecin derivatives[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2005,15(13):3233-3236.
APA	Gao, HY.,Zhang, XW.,Chen, Y.,Shen, HW.,Pang, T.,...&Lu, W.(2005).Synthesis and antitumor activity of the hexacyclic camptothecin derivatives.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,15(13),3233-3236.
MLA	Gao, HY,et al."Synthesis and antitumor activity of the hexacyclic camptothecin derivatives".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 15.13(2005):3233-3236.