Phenylahistin,a small dipeptidic colchicine-like anti-microtubule agent:total synthesis and SAR study of the derivatives

摘要

Phenylahistin (1),a fungal metabolite from Aspergillus ustus NSC-F038,belongs to a new class of peptidic colchicine-like microtubule-binding agents that exhibits cytotoxic activity against a wide variety of tumor cells lines.(-)-Phenylahistin-(-)-1,a diketopiperazine derivative,consists of L-phenylamine and a unique isoprenylated dehydrohistidine residue with a quaternary carbon at the 5-position of the imidazole ring.