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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Developments of Combretastatin A-4 Derivatives as Anticancer Agents

Author(s): Y. Shan Shan, J. Zhang, Z. Liu, M. Wang and Y. Dong

Volume 18 , Issue 4 , 2011

Page: [523 - 538] Pages: 16

DOI: 10.2174/092986711794480221

Price: $65


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, 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

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