676629-08-6Relevant articles and documents
Tubulin inhibitors. Synthesis and biological activity of HTI-286 analogs with B-segment heterosubstituents
Niu, Chuan,Smith, Daniel,Zask, Arie,Loganzo, Frank,Discafani, Carolyn,Beyer, Carl,Greenberger, Lee,Ayral-Kaloustian, Semiramis
, p. 4329 - 4332 (2007/10/03)
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.