Structural modifications on the phenazine N, N′-dioxide-scaffold looking for new selective hypoxic cytotoxins

ML Lavaggi, M Nieves, M Cabrera, C Olea-Azar…

Index: Lavaggi, Maria Laura; Nieves, Marcos; Cabrera, Mauricio; Olea-Azar, Claudio; Lopez De Cerain, Adela; Monge, Antonio; Cerecetto, Hugo; Gonzalez, Mercedes European Journal of Medicinal Chemistry, 2010 , vol. 45, # 11 p. 5362 - 5369

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Citation Number: 15

Abstract

We have identified phenazine 5, 10-dioxides as prodrugs for antitumour therapy that undergo hypoxic-selective bioreduction to form cytotoxic species. Here, we investigated some structural modifications in order to find new selective hypoxic cytotoxins and to establish the structural requirements for adequate activity. Three different chemical-series were prepared and the clonogenic survival of V79 cells on aerobic and anaerobic ...