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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

DOI: 10.1016/s0960-894x(03)00534-1