Synthesis and cytotoxic activity of a new series of topoisomerase I inhibitors

S Dallavalle, S Gattinoni, S Mazzini, L Scaglioni…

Index: Dallavalle, Sabrina; Gattinoni, Sonia; Mazzini, Stefania; Scaglioni, Leonardo; Merlini, Lucio; Tinelli, Stella; Beretta, Giovanni L.; Zunino, Franco Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 4 p. 1484 - 1489

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Citation Number: 20

Abstract

A series of structurally simple analogues of natural topopyrone C were synthesized and tested for cytotoxic and topoisomerase I inhibitory activities. The removal of the hydroxyl groups at the 5 and 9 positions resulted in an increased cytotoxic potency and ability to stabilize topoisomerase-mediated cleavage. In addition, the results suggest that some structural features, such as the pyrone ring and a polar group in position 11, are ...