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Syntheses and biological evaluation of ring-C modified colchicine analogs.

Abstract：

:Ring-C modified alkaloids were synthesized from colchicine using iminonitroso Diels-Alder reactions in a highly regio- and stereoselective fashion. Several analogs exhibited cytotoxic activity similar to that of colchicine itself against PC-3 and MCF-7 cancer cell lines, by serving as prodrugs of colchicine through retro Diels-Alder reactions under the assayed conditions. In vitro microtubule polymerization assays indicated that these modifications affected their interaction with tubulin.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Yang B,Zhu ZC,Goodson HV,Miller MJ

doi

10.1016/j.bmcl.2010.03.056

subject

Has Abstract

pub_date

2010-06-15 00:00:00

pages

3831-3

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00377-X

journal_volume

20

pub_type

杂志文章

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