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Substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones and analogues: synthesis, cytotoxic activity, and study of the mechanism of action.

Abstract：

:The synthesis of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones and analogues is reported. Their cytotoxic activity was evaluated according to protocols available at the National Cancer Institute (NCI), Bethesda, MD. The action of selected compounds was examined for potential inhibition of tubulin assembly in comparison with the potent colchicine site agent combretastatin A-4. The most potent compounds also strongly and selectively inhibited the phosphorylation of the oncoprotein kinase Akt in cancer cells. The effect of the most interesting compounds was examined on the growth of HT-29 colon cancer cells. These compounds caused the cells to arrest in the G2/M phase of the cell cycle, as would be expected for inhibitors of tubulin assembly.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Andreani A,Granaiola M,Locatelli A,Morigi R,Rambaldi M,Varoli L,Calonghi N,Cappadone C,Farruggia G,Stefanelli C,Masotti L,Nguyen TL,Hamel E,Shoemaker RH

doi

10.1021/jm2012694

subject

Has Abstract

pub_date

2012-03-08 00:00:00

pages

2078-88

issue

5

eissn

0022-2623

issn

1520-4804

journal_volume

55

pub_type

杂志文章

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