Tubulin inhibitors. Synthesis and biological activity of HTI-286 analogs with B-segment heterosubstituents

…, C Beyer, L Greenberger, S Ayral-Kaloustian

Index: Niu, Chuan; Smith, Daniel; Zask, Arie; Loganzo, Frank; Discafani, Carolyn; Beyer, Carl; Greenberger, Lee; Ayral-Kaloustian, Semiramis Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 16 p. 4329 - 4332

Full Text: HTML

Citation Number: 9

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 ...