Review Article

Cellular Cofactors of Lentiviral Integrase: From Target Validation to Drug Discovery

Figure 3

Chemical structures of the LEDGINs. Of the 25 molecules tested in AlphaScreen, compound 1 was identified as the initial hit with in vitro activity. Compounds 2 and 3 are commercial congeners of 1. Compounds 4ā€“7 are newly synthesized compounds with improved in vitro and in vivo activities. After serial rounds of optimization by medicinal chemistry, the early lead compounds 6 and 7 were identified with potent and selective anti-HIV activity. Compound 7 has submicromolar antiviral activity [37].
863405.fig.003