Author: Nam Nguyen-Hai

Source: Current Medicinal Chemistry, Volume 10, Number 17, September 2003 , pp. 1697-1722(26)

Publisher: Bentham Science Publishers

Abstract:

Tubulin protein is a major target for anticancer drug discovery. As a result, antimitotic agents constitute an important class of the current anticancer drugs. Hundreds of tubulin inhibitors, naturally occurring, semisynthetic or synthetic, have been reported. Among these, combretastatin A-4 (CA-4), isolated from a South African tree Combretum caffrum, is one of the most potent antimitotic agents. CA-4 shows strong cytotoxicity against a variety of cancer cells, including multi-drug resistant cancer cell lines. It has also been demonstrated to exert highly selective effects in proliferating endothelial cells. CA-4 disodium phosphate (CA4DP), a water-soluble prodrug of CA- 4, shows potent antivascular and antitumor effects in a wide variety of preclinical tumor models. Consequently, a number of CA-4 analogues has been synthesized and evaluated. In this paper, the structure-activity relationships and pharmacological properties of the CA-4 derivatives as a class of potent antimitotic anticancer agents are reviewed and discussed.

Keywords: combretastatin a-4; combretum caffrum; structure-activity relationships; antimitotic agents; antivascular activity

Document Type: Review article

DOI: http://dx.doi.org/10.2174/0929867033457151

Affiliations: 1: Department of Biomedical Sciences, University of Rhode Island, 41-Fogarty Hall, Lower College Road, Kingston, RI 02881, USA.

Publication date: 2003-09-01

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• Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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