Synthesis and SAR study of acridine, 2-methylquinoline and 2-phenylquinazoline analogues as anti-prion agents

H Cope, R Mutter, W Heal, C Pascoe, P Brown…

Index: Cope; Mutter; Heal; Pascoe; Brown; Pratt; Chen European Journal of Medicinal Chemistry, 2006 , vol. 41, # 10 p. 1124 - 1143

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Citation Number: 37

Abstract

Transmissible spongiform encephalopathies (TSEs) are thought to arise from aggregation of a protease resistant protein denoted PrPSc, which is a misfolded isoform of the normal cellular prion protein PrPC. Using virtual high-throughput screening we have selected structures analogous to acridine, 2-methyquinoline and 2-phenylquinazoline as potential therapeutic candidates for the treatment of TSEs. From the synthesis and screening of ...