Author/Authors :
Chuan Niu، نويسنده , , Daniel Smith، نويسنده , , Arie Zask، نويسنده , , Frank Loganzo، نويسنده , , Carolyn Discafani، نويسنده , , Carl Beyer، نويسنده , , Lee Greenberger، نويسنده , , Semiramis Ayral-Kaloustian، نويسنده ,
Abstract :
Modifications of the B-segment of HTI-286 (2) produced a class of analogs incorporating heteroatom-substituents. The structure–activity relationship was studied. Analogs bearing methylsulfide and fluoride groups exhibited potency comparable to that of the parent compound HTI-286 and to paclitaxel in cytotoxicity assays against KB-3-1 cell lines. These analogs were more potent than paclitaxel against P-glycoprotein expressing KB-8-5 and KB-V1 cell lines. Several analogs showed strong inhibition of tubulin polymerization.
