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1. Synthesis and biological evaluation of C-13 amide-linked paclitaxel (Taxol) analogs

Author

Chen, Shu-Hui, Farina, Vittorio, Vyas, Dolatrai M., Doyle, Terrence W., Long, Byron H., and Fairchild, Craig

Subjects
Tubulins -- Research, Amides -- Research, Structure-activity relationship (Pharmacology) -- Methods, Organic compounds -- Synthesis, Serum -- Research, Biological assay -- Methods, Biological sciences, Chemistry
Abstract

A new series of C-13 amido-containing paclitaxel analogs were accidentally synthesized during structure-activity relationship tests of paclitaxel (Taxol), an antitumor drug from Bristol-Myers Squibb. The analogs included 4-deacetyl-13-amidopaclitaxel, 13-amidopaclitaxel 4-(methyl carborate) derivatives, and 13-amidopaclitaxel. Biological profiling assays, in tubulin polymerization and in vitro cytoxicity assay against a human colon cancer cell line, determined the nonreactivity of the analogs.

Published
1996

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