Enantioselective Total Synthesis of Bistramide A

摘要

Bistramide A~1(1)is a member of a new class of bioactive molecules isolated from the marine ascidian Lissoclinum bistratum.The bistramides demonstrate significant neuro-and cytotoxic properties as well as profound effects on cell cycle regulation.In particular,bistramide A has an IC_(50)of 0.03-0.32 mug/mL for the P388/dox,B16,HT29,and NSCLC-N6 cell lines.Studies have shown that bistramide A is cell permeable,blocks sodium channels,and induces highly selective activation of a single protein kinase C(PKC)isotype delta.The biological activity of bistramide A,as well as the other bistramides,has rendered them potential candidates for the treatment of slowly evolving tumors,such as nonsmall cell pulmonary carcinoma.