| Literature DB >> 9733497 |
D G Kingston1, A G Chaudhary, M D Chordia, M Gharpure, A A Gunatilaka, P I Higgs, J M Rimoldi, L Samala, P G Jagtap, P Giannakakou, Y Q Jiang, C M Lin, E Hamel, B H Long, C R Fairchild, K A Johnston.
Abstract
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.Entities:
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Year: 1998 PMID： 9733497 DOI： 10.1021/jm980229d
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446