Document Report Card

ID: ALA1130998

Journal: J Med Chem

Title: Structure-activity requirements for flavone cytotoxicity and binding to tubulin.

Authors: Beutler JA, Hamel E, Vlietinck AJ, Haemers A, Rajan P, Roitman JN, Cardellina JH, Boyd MR.

Abstract: A series of 79 flavones related to centaureidin (3,6,4'-trimethoxy-5, 7,3'-trihydroxyflavone, 1) was screened for cytotoxicity in the NCI in vitro 60-cell line human tumor screen. The resulting cytotoxicity profiles of these flavones were compared for degree of similarity to the profile of 1. Selected compounds were further evaluated with in vitro assays of tubulin polymerization and [3H]colchicine binding to tubulin. Maximum potencies for tubulin interaction and production of differential cytotoxicity profiles characteristic of 1 were observed only with compounds containing hydroxyl substituents at C-3' and C-5 and methoxyl groups at C-3 and C-4'.

CiteXplore: 9632366

DOI: 10.1021/jm970842h