Document Report Card
Basic Information
ID: ALA1136159
Journal: Bioorg Med Chem Lett
Title: Synthesis and pharmacological evaluation of novel non-lactone analogues of camptothecin.
Authors: Hautefaye P, Cimetière B, Pierré A, Léonce S, Hickman J, Laine W, Bailly C, Lavielle G.
Abstract: Ten novel camptothecin (CPT) derivatives devoid of the lactone function in the E-ring were synthesized and evaluated as anticancer agents. Several of these CPT analogues bearing a five-membered E-ring are potent inhibitors of the DNA relaxation and cleavage reactions catalyzed by topoisomerase I and exhibit promising cytotoxic activities with IC(50) values in the nM range. This is the first successful design of lactone-free CPT, providing thus a new avenue to the development of topoisomerase I targeted antitumor agents.
CiteXplore: 12873503