| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371066 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
A novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) combinatory library was synthesized and evaluated with C8166 cells infected by the HIV-1IIIB 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 EC50 values of 0.012, 0.025, 0.088 and 0.162 nM, respectively.
Graphical abstractA series of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) were designed, synthesized and evaluated for anti-HIV-1 activity in vitro.Figure optionsDownload full-size imageDownload as PowerPoint slide
