Synthesis and biological evaluation of 2-acyl analogues of paclitaxel (Taxol).
نویسندگان
چکیده
The anticancer drug paclitaxel (Taxol) has been converted to a large number of 2-debenzoyl-2-aroyl derivatives by three different methods. The bioactivities of the resulting analogues were determined in both tubulin polymerization and cytotoxicity assays, and several analogues with enhanced activity as compared with paclitaxel were discovered. Correlation of cytotoxicity in three cell lines with tubulin polymerization activity showed reasonable agreement. Among the cell lines examined, the closest correlation with antitubulin activity was observed with a human ovarian carcinoma cell line.
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ورودعنوان ژورنال:
- Journal of medicinal chemistry
دوره 41 19 شماره
صفحات -
تاریخ انتشار 1998