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

  • Bioorg Med Chem Lett. 2011 Jan 15;21(2):694-7. doi: 10.1016/j.bmcl.2010.12.003.
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
  • 1. Key Laboratory of Medicinal Chemistry for Natural Resource Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China. [email protected]
PMID: 21194939 DOI: 10.1016/j.bmcl.2010.12.003
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.