BPR0C305, an orally active microtubule-disrupting anticancer agent.

Abstract:

:BPR0C305 is a novel N-substituted indolyl glyoxylamide previously reported with in-vitro cytotoxic activity against a panel of human cancer cells including P-gp-expressing multiple drug-resistant cell sublines. The present study further examined the underlying molecular mechanism of anticancer action and evaluated the in-vivo antitumor activities of BPR0C305. BPR0C305 is a novel synthetic small indole derivative that demonstrates in-vitro activities against human cancer cell growth by inhibiting tubulin polymerization, disrupting cellular microtubule assembly, and causing cell cycle arrest at the G2/M phase. It is also orally active against leukemia and solid tumor growths in mouse models. Findings of these pharmacological and pharmacokinetic studies suggest that BPR0C305 is a promising lead compound for further preclinical developments.

journal_name

Anticancer Drugs

journal_title

Anti-cancer drugs

authors

Li WT,Yeh TK,Song JS,Yang YN,Chen TW,Lin CH,Chen CP,Shen CC,Hsieh CC,Lin HL,Chao YS,Chen CT

doi

10.1097/CAD.0000000000000014

subject

Has Abstract

pub_date

2013-11-01 00:00:00

pages

1047-57

issue

10

eissn

0959-4973

issn

1473-5741

journal_volume

24

pub_type

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