BPR0C305, an orally active microtubule-disrupting anticancer agent

Wen Tai Li*, Teng Kuang Yeh, Jen Shin Song, Yung Ning Yang, Tung Wei Chen, Chi Hung Lin, Ching Ping Chen, Chien Chang Shen, Chih Chien Hsieh, Heng Liang Lin, Yu Sheng Chao, Chiung Tong Chen

*Corresponding author for this work

Research output: Contribution to journalArticle

1 Scopus citations

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.

Original languageEnglish
Pages (from-to)1047-1057
Number of pages11
JournalAnti-Cancer Drugs
Volume24
Issue number10
DOIs
StatePublished - Nov 2013

Keywords

  • microtubule
  • N-substituted indolyl glyoxylamide
  • pharmacokinetics
  • tubulin

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