676629-31-5

Upstream product

• 228266-38-4 N-(tert-butoxycarbonyl)-N,β,β-trimethyl-L-phenylalanine 
• 676629-25-7 (E)-(S)-4-{[(S)-2-tert-Butoxycarbonylamino-3-(4-methoxy-phenyl)-3-methyl-butyryl]-methyl-amino}-2,5-dimethyl-hex-2-enoic acid ethyl ester 
• 676631-15-5 2-tert-butoxycarbonylamino-3-(4-methoxy-phenyl)-3-methyl-butyric acid 

Relevant academic research and scientific papers

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

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.