Document Report Card

ID: ALA1148704

Journal: J Med Chem

Title: First total synthesis of protoapigenone and its analogues as potent cytotoxic agents.

Authors: Lin AS, Nakagawa-Goto K, Chang FR, Yu D, Morris-Natschke SL, Wu CC, Chen SL, Wu YC, Lee KH.

Abstract: Protoapigenone (1), isolated from Thelypteris torresiana, previously showed significant cytotoxic activity against five human cancer cell lines. In a continued structure-activity relationship study, the first total synthesis and modification of 1 were achieved. All synthesized compounds and related intermediates were evaluated for cytotoxic activity against five human cancer cell lines, HepG2, Hep3B, MDA-MB-231, MCF-7, and A549. Among them, 24 showed 2.2-14.2-fold greater cytotoxicity than 1 and naphthyl A-ring analogues remarkably enhanced the activity.

CiteXplore: 17622129

DOI: 10.1021/jm070363a