Authors: Shan, Y. Shan; Zhang, J.; Liu, Z.; Wang, M.; Dong, Y.

Source: Current Medicinal Chemistry, Volume 18, Number 4, February 2011 , pp. 523-538(16)

Publisher: Bentham Science Publishers

Abstract:

Tubulin protein is one of several members of a small family of globular proteins. It offers a potential target for anticancer drug design and development. Combretastatin A-4 (CA-4) is a potent anticancer and antiangiogenesis natural substance isolated from Combretum caffrum. Modifications on the CA-4 structure have led to a great number of novel CA-4 derivatives as potent tubulin inhibitors and high cytotoxic anticancer agents is becoming an interesting field, leading to a breakthrough in the treatment of cancer. In this review, the recent developments of novel CA-4 derivatives via the modifications on the A- and B-ring and the double bond as anticancer agents are discussed.

Keywords: Combretastatin A-4; Tubulin inhibitors; Anticancer; Antineoplastic Agents; Structure-Activity Relationships; antiangiogenesis; Combretum caffrum; chromo-somes; mitosis; microtu-bules; apoptosis; colchicine; vinca alka-loid domain; vinblastine; vincristine; Combretastatins; stilbenoid phenol; Combretum caffrum; tubulin polymerization; chemotherapeutic; structure-activity relationship (SAR); human myelogenous leukaemia cell line; phosphate diesters; carcinoma; pinacolylboronate; boronic acid; Ethene Bridge; olefinic bridge; antineoplastic activity; hyperploid

Document Type: Research article

DOI: http://dx.doi.org/10.2174/092986711794480221

Publication date: 2011-02-01

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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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