The chemistry of taxol and related taxoids.

作者: D. G. I. Kingston , P. G. Jagtap , H. Yuan , L. Samala

DOI: 10.1007/978-3-7091-6160-9_2

关键词:

摘要: The anticancer compound taxol (1.1.1) was originally isolated in the late 1960’s from bark of Western Yew, Taxus brevifolia, and its structure published 1971 a paper that has been cited well over 1000 times since publication (1). Taxol on basis cytotoxicity antileukemic activity, but it not actively developed as drug for several years because scarcity (the initial yield yew 0.02%) lack water-solubility. Fortunately additional testing at National Cancer Institute revealed activity against various human solid tumor xenografts nude mice, program to develop initiated 1977. A key discovery Horwitz laboratory 1979, also publication, showed had unique mechanism action, binding polymerized tubulin stabilizing microtubules dissociation (2). These twin discoveries taxol’s action provided impetus continued clinical trials face some disappointments, first positive results ovarian cancer were announced 1989 (3). Following these found be effective breast (4) licensed Bristol-Myers Squibb; sales are estimated $1.6 billion 2000 (5).

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