Author/Authors :
Iwao Ojima، نويسنده , , Songnian Lin، نويسنده , , John C Slater، نويسنده , , Tao Wang، نويسنده , , Paula Pera، نويسنده , , Ralph J. Bernacki، نويسنده , , Cristiano Ferlini، نويسنده , , Giovanni Scambia، نويسنده ,
Abstract :
A series of new taxoids bearing difluoromethyl group at the C-3′ position and modifications at the C-10 and C-14 positions has been synthesized and their biological activities studied. The in vitro cytotoxicity assay results indicate that these newly developed taxoids exhibit comparable to several times better activity against drug-sensitive cell line LCC6-WT, and 40–70 times better activity against the corresponding drug-resistant cancer cell line LCC6-MDR as compared to that of paclitaxel. Apoptosis analysis has revealed the exceptional activity of SB-T-12843 (1e) in inducing apoptosis in both MDR-bearing and MDR-negative cancer cells.
