Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position

T Nguyen, Y Sakasegawa, K Doh-ura, ML Go

文献索引：Nguyen, Thuy; Sakasegawa, Yuji; Doh-Ura, Katsumi; Go, Mei-Lin European Journal of Medicinal Chemistry, 2011 , vol. 46, # 7 p. 2917 - 2929

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被引用次数: 15

摘要

Abstract In this paper, we report the synthesis and cell-based anti-prion activity of quinacrine analogs derived by replacing the basic alkyl side chain of quinacrine with 4-(4- methylpiperazin-I-yl) phenyl,(1-benzylpiperidin-4-yl) and their structural variants. Several promising analogs were found that have a more favorable anti-prion profile than quinacrine in terms of potency and activity across different prion-infected murine cell models. They ...