2006ChemMedChemRequires access

Cover Picture: Molecular Design and Chemical Synthesis of a Highly Potent Epothilone (ChemMedChem 1/2006)

K. C. Nicolaou, Benjamin A. Pratt, Stellios Arseniyadis, Markus Wartmann, Aurora O’Brate, Paraskevi Giannakakou

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Abstract

The cover picture shows a potent epothilone derivative with a schematized tubulin microtubule in the background. Epothilones exert their antitumor activity through the stabilization of microtubules by binding with tubulin; cell division stops if microtubules cannot disassemble properly. The structure shown here is the most potent epothilone reported to date. It is more potent than epothilone B in a wide range of cancer cell types, and shows excellent promise against taxol‐ and epothilone A‐resistant cell lines. For more details, see the communication by K. C. Nicolaou et al. on p. 41 ff.

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What this paper is about

The cover picture shows a potent epothilone derivative with a schematized tubulin microtubule in the background. Epothilones exert their antitumor activity through the stabilization of microtubules by binding with tubulin; cell division stops if microtubules cannot disassemble properly. The structure shown here is the most potent epothilone reported to date. It is more potent than epothilone B in a wide range of cancer cell types, and shows excellent promise against taxol‐ and epothilone A‐resistant cell lines. For more details, see the communication by K. C. Nicolaou et al. on p. 41 ff.

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Available abstract

The cover picture shows a potent epothilone derivative with a schematized tubulin microtubule in the background. Epothilones exert their antitumor activity through the stabilization of microtubules by binding with tubulin; cell division stops if microtubules cannot disassemble properly. The structure shown here is the most potent epothilone reported to date. It is more potent than epothilone B in a wide range of cancer cell types, and shows excellent promise against taxol‐ and epothilone A‐resistant cell lines. For more details, see the communication by K. C. Nicolaou et al. on p. 41 ff.

Key concepts: Epothilones, Epothilone, Tubulin, Microtubule, Ixabepilone, Chemistry, Stereochemistry, Computational biology

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