Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis and In Vitro Biological Activity Evaluation of the Derivatives of Combretastatin A-4

Author(s): Zhaoqi Yang.

Abstract:

Combretastatin A-4 (CA-4) is a potent anti-tumor agent, which strongly inhibits tubulin polymerization. A common problem is the inactivation of derivatives with cis-configurated ethylene bridges during storage. β-Lactam analogs of CA-4 were synthesized in order to avoid isomerization to E-forms. Moreover, B-ring modifications (3,4,5-trimethoxyphenyl ring, furan ring) were studied with regard to biological activity. Their cytotoxic effects were evaluated in vitro against L1210 leukemia cell. The derivatives might provide some rational basis for further optimal structural modification.

Keywords: CA-4, Synthesis, Derivatives, Anti-tumor

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Article Details

VOLUME: 3
ISSUE: 8
Year: 2006
Page: [544 - 546]
Pages: 3
DOI: 10.2174/157018006778194727
Price: $58