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. 2011 Jan 15;21(2):694-7.
doi: 10.1016/j.bmcl.2010.12.003. Epub 2010 Dec 7.

Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents

Yan-Ping He  1 , 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
Affiliations

Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents

Yan-Ping He et al. Bioorg Med Chem Lett. .

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.

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