Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs.

Abstract:

:In an effort to discover potent antitumor agents, a series of novel C-7-heteroaryl-substituted camptothecin derivatives were designed and synthesized via microwave-promoted Suzuki coupling reaction. These analogs were then assessed for cytotoxicity against three human tumor cell lines, A549, HCT116, HT-29, and inhibitory effects on topoisomerase I. All of the new compounds showed potent inhibition of human tumor cell growth, among which compound 10a showed higher cytotoxic activity than that of SN-38. Furthermore, this series of compounds retained or enhanced Topo I inhibition.

journal_name

Bioorg Med Chem Lett

authors

Wang L,Huang Y,Zhang J,Tong L,Chen Y,Lu W,Huang Q

doi

10.1016/j.bmcl.2014.01.049

subject

Has Abstract

pub_date

2014-03-15 00:00:00

pages

1597-9

issue

6

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)00079-1

journal_volume

24

pub_type

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