The chemistry and biology of antimitotic chalcones and related enone systems.
The development of combretastatin as an antimitotic agent has led to an enormous effort to design other tubulin-targeting agents. The intriguing discovery that combretastatin A-4 phosphate causes selective damage to tumor vasculature has stimulated even more activity in this field. This attention to tubulin binding agents and their antivasculature activity is highly likely to lead to significant clinical advances for the treatment of cancer. This review focuses on the development of ketones as tubulin-binding agents such as chalcones and related enones as surrogates of combretastatin and colchicine.
Lawrence
Nicholas J
NJ
Drug Discovery Program, H. Lee Moffitt Cancer Center & Research Institute, Department of Interdisciplinary Oncology, University of South Florida, Tampa, Florida 33612, USA. Lawrennj@moffitt.usf.edu
McGown
Alan T
AT
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D001577:Benzophenones / Q000737:chemistry; D002599:Chalcone / Q000737:chemistry* / Q000494:pharmacology; D003078:Colchicine / Q000737:chemistry; D003460:Crystallization; D015195:Drug Design; D047309:Flavones / Q000737:chemistry; D014404:Tubulin / Q000378:metabolism; D014961:X-Ray Diffraction
D000970:Antineoplastic Agents; D001577:Benzophenones; D047309:Flavones; D014404:Tubulin; D002599:Chalcone; D003078:Colchicine