Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs

…, X Chen, P Zhan, E De Clercq, C Pannecouque…

文献索引：Rai, Diwakar; Chen, Wenmin; Tian, Ye; Chen, Xuwang; Zhan, Peng; De Clercq, Erik; Pannecouque, Christophe; Balzarini, Jan; Liu, Xinyong Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 23 p. 7398 - 7405

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被引用次数: 2

摘要

Abstract A novel series of 3-benzyloxy-linked pyrimidinylphenylamine derivatives (8a–8s) was designed, synthesized and evaluated for their in vitro anti-HIV activity in MT-4 cell cultures. Most of the compounds inhibited wild-type (wt) HIV-1 replication in the lower micromolar concentration range (EC 50= 0.05–35 μM) with high selectivity index (SI) values (ranged from 10 to> 4870). In particular, 8h and 8g displayed excellent antiretroviral ...