Total synthesis and cytotoxicity of bisebromoamide and its analogues

A highly convergent route for assembling bisebromoamide, its stereoisomers and a simplified analogue has been accomplished, which features connecting its left part and right part via thiazoline ring formation at the final stage. Preliminary biological studies revealed that compounds with both proposed and revised structures, and a simplified analogue have similar potency against the proliferation of HeLa S-3 cell, indicating that the stereochemistry of methylthiazoline part, and methyl group at the 4-methylproline residue in bisebromoamide, have limited influence on its cytotoxicity. (C) 2010 Elsevier Ltd. All rights reserved.