Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3, 4-dihydroquinolin-1 (2H)-yl) methyl) pyrimidin-4 (3H)-ones as potent non-nucleoside HIV-1 …

…, Y Jiang, W Ge, C Pannecouque, E De Clercq…

Index: Zhang, Jing; Zhan, Peng; Wu, Jingde; Li, Zhenyu; Jiang, Yan; Ge, Weiying; Pannecouque, Christophe; De Clercq, Erik; Liu, Xinyong Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 14 p. 4366 - 4376

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Citation Number: 14

Abstract

Abstract A series of novel S-DABO analogues of 5-alkyl-2-arylthio-6-((3, 4-dihydroquinolin-1 (2H)-yl) methyl) pyrimidin-4 (3H)-ones were synthesized and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). Among them, the most potent HIV-1 inhibitors were compounds 6c1, 6c6, and 6b1 (EC 50= 0.24±0.05, 0.38±0.13, 0.39±0.05 μM, respectively), which possess improved or similar HIV-1 inhibitory activity compared with ...