Synthesis and Biological Evaluation of 2-Acyl Analogues of Paclitaxel (Taxol)

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• 作者：David G. I. Kingston ; Ashok G. Chaudhary ; Mahendra D. Chordia ; Milind Gharpure ; A. A. Leslie Gunatilaka ; Paul I. Higgs ; John M. Rimoldi ; Lakshman Samala ; Prakash G. Jagtap ; Paraskevi Giannakakou ; Yuan
• 刊名：Journal of Medicinal Chemistry
• 出版年：1998
• 出版时间：September 10, 1998
• 年：1998
• 卷：41
• 期：19
• 页码：3715 - 3726
• 全文大小：204K
• 年卷期：v.41,no.19(September 10, 1998)
• ISSN：1520-4804

文摘

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 analogueswere determined in both tubulin polymerization and cytotoxicity assays, and several analogueswith enhanced activity as compared with paclitaxel were discovered. Correlation of cytotoxicityin three cell lines with tubulin polymerization activity showed reasonable agreement. Amongthe cell lines examined, the closest correlation with antitubulin activity was observed with ahuman ovarian carcinoma cell line.