Drugs that Inhibit Tubulin Polymerization: The Particular Case of Podophyllotoxin and Analogues

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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Drugs that Inhibit Tubulin Polymerization: The Particular Case of Podophyllotoxin and Analogues



Anti-Cancer Agents in Medicinal Chemistry, 2(1): 71-90.

Author(s): Stephanie Desbene and Sylviane Giorgi-Renault.

Affiliation: Laboratoire de Chimie Therapeutique, UMR CNRS-Universite Rene Descartes N o 8638, Faculte des Sciences Pharmaceutiques et Biologiques, 4 avenue de l'Observatoire, 75270 Paris Cedex 06, France

Abstract

Tubulin being a major cellular target for antitumor drugs, tubulin-interacting compounds have attracted great attention as antimitotic agents. Two main classes of antimitotic drugs are known and one of them includes podophyllotoxin, a natural product. The clinical use of podophyllotoxin in the treatment of cancer has been limited by severe toxic side effects. In an attempt to find less toxic analogues, many podophyllotoxin derivatives have been prepared. Identification of two types of mechanisms of action has led to the development of two groups of podophyllotoxin analogues: tubulin polymerisation inhibitors and topoisomerase II inhibitors. The present article focuses on the first group of podophyllotoxin analogues i.e. those that retain “podophyllotoxin-like” activity. The review starts with a short summary of the structural characteristics of tubulin and its interactions with drugs that affect the microtubule dynamics and then deals with the particular case of podophyllotoxin. Particula r attention is given to the nature and the location of the binding sites compared to those of colchicine. The main purpose of the present review being the search for structure-activity relationships, the structural significant features required for antitubulin activity are described and discussed in details.

Keywords:

Tubulin Polymerization, podophyllotoxin, Etoposide, Teniposide, Microtubules, Antimitotic agent, Colchicines, Stegnacin, Combrestatins.



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Article Details

Volume: 2
Issue Number: 1
First Page: 71
Last Page: 90
Page Count: 20
DOI: 10.2174/1568011023354353
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