| Literature DB >> 21194939 |
Yan-Ping He1, Jin Long, Shui-Shuan Zhang, Cong Li, Christopher Cong Lai, Chun-Sheng Zhang, Da-Xiong Li, De-Hua Zhang, Hua Wang, Qing-Qing Cai, Yong-Tang Zheng.
Abstract
A novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) combinatory library was synthesized and evaluated with C8166 cells infected by the HIV-1(IIIB) in vitro, using Nevirapine (NVP) and Zidovudine (AZT) as positive control. The anti-HIV screening results revealed that C-6-cyclohexylmethyl substituted pyrimidinones possessed higher selective index than its 6-arylmethyl counterparts. Compounds 1g, 1c, 1e and 1b showed potent anti-HIV activities with EC(50) values of 0.012, 0.025, 0.088 and 0.162nM, respectively. Copyright ÂEntities:
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Year: 2010 PMID： 21194939 DOI： 10.1016/j.bmcl.2010.12.003
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823