Preparation and biological activity of taxol acetates |
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Authors: | Wilfredo Mellado Neal F. Magri David G.I. Kingston Renee Garcia-Arenas George A. Orr Susan Band Horwitz |
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Affiliation: | 1. Department of Molecular Pharmacology, Albert Einstein College of Medicine, 1300 Morris Park Avenue, Bronx, NY 10461 USA;2. Department of Chemistry, Virginia Polytechnic Institute and State University, Blacksburg, VA 24061 USA |
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Abstract: | Synthesis and biological activity of 2′-acetyltaxol and 7-acetyltaxol are reported. Activity is measured by cytotoxicity toward the macrophage-like cell line J774.2, and by promotion of microtubule assembly in the absence of exogenous GTP. Addition of an acetyl moiety at C-2′ results in loss of activity but not cytotoxicity. The properties of 7-acetyltaxol are similar to those of taxol in its effects on cell replication and on microtubule polymerization. Therefore a free hydroxyl group at C-7 is not required for activity and this position is available for structural modifications. |
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