1.
Fortschr Chem Org Naturst
; 84: 53-225, 2002.
Artículo
en Inglés
| MEDLINE
| ID: mdl-12132389
2.
J Med Chem
; 41(19): 3715-26, 1998 Sep 10.
Artículo
en Inglés
| MEDLINE
| ID: mdl-9733497
RESUMEN
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.