E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation

…, E Marastoni, G Battistuzzi, L Vesci, C Pisano…

Index: Giannini, Giuseppe; Marzi, Mauro; Cabri, Walter; Marastoni, Elena; Battistuzzi, Gianfranco; Vesci, Loredana; Pisano, Claudio; Beretta, Giovanni Luca; Cesare, Michelandrea De; Zunino, Franco Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 9 p. 2910 - 2915

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Citation Number: 10

Abstract

In contrast to five-membered E-ring analogues, 7-oxyiminomethyl derivatives of homocamptothecins showed ability to form stable ternary complexes with DNA and topoisomerase I. The 7-oxyiminomethyl derivatives of homocamptothecins were evaluated as a racemic mixture. Following the isolation of the two enantiomers, the 20 (R)-hydroxy isomer confirms the best activity. By using a panel of human tumor cells, all tested ...