Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase

…, S Bongarzone, R Brun, RL Krauth-Siegel…

Index: Cavalli, Andrea; Lizzi, Federica; Bongarzone, Salvatore; Brun, Reto; Luise Krauth-Siegel; Bolognesi, Maria Laura Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 11 p. 3031 - 3035

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Citation Number: 30

Abstract

Novel quinazoline-type compounds were designed as inhibitors of the parasite specific enzyme trypanothione reductase (TR), and their biological activities were evaluated. Some of our compounds inhibited TR, showed selectivity for TR over human glutathione reductase, and inhibited parasite growth in vitro. We propose that the quinazoline framework is a privileged structure that can be purposely modified to design novel TR inhibitors. ...