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Indole, a core nucleus for potent inhibitors of tubulin polymerization
Author(s) -
Brancale Andrea,
Silvestri Romano
Publication year - 2007
Publication title -
medicinal research reviews
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.868
H-Index - 130
eISSN - 1098-1128
pISSN - 0198-6325
DOI - 10.1002/med.20080
Subject(s) - tubulin , indole test , microtubule , chemistry , nucleus , polymerization , microtubule polymerization , stereochemistry , biophysics , biochemistry , biology , microbiology and biotechnology , organic chemistry , polymer
Microtubules are the basic components of cell structure, which take part in a wide number of pivotal cellular functions. Drugs that are able to modulate the microtubule assembly either by inhibition of tubulin polymerization or by blocking microtubule disassembly are of great interest in anti‐cancer therapy. Several tubulin polymerization inhibitors characterized by the presence of an indole nucleus have been obtained from natural sources or have been prepared by semi‐synthesis. In the last decade an ever increasing number of synthetic indoles have been reported. We have reviewed anti‐tubulin agents obtained by synthesis having an indole as core nucleus. The synthesis, the biological activity, and the structure–activity relationship aspects of 3‐formyl‐2‐phenylindoles, heterocombretastatins, diarylindoles, 2‐aroylindoles, D‐24851, 2‐aryl‐3‐aroylindoles, 3‐aroyl‐ and 1‐aroylindoles, and arylthioindoles are discussed. © 2006 Wiley Periodicals, Inc. Med Res Rev