"New Alkenyldiarylmethanes With Enhanced Potencies as Anti-HIV Agents Which Act as Non-Nucleoside Reverse Transcriptase Inhibitors."

According to the authors' abstract of an article published in Journal of Medicinal Chemistry, "Twenty-two new alkenyldiarylmethanes (ADAMs) were synthesized and evaluated for inhibition of HIV-1 replication. The most potent compound proved to be methyl 3',3 '-dichloro-4',4 '-dimethoxy-5', 5 '-bis(methoxycarbonyl)-6, (ADAM II), which displayed an EC₅₀ of 13 nM for inhibition of the cytopathic effect of HIV-1(RF) in CEM-SS cells. ADAM II inhibited HIV-1 reverse transcriptase with an IC₅₀ of 0.3 (mu)M but was inactive as an inhibitor of HIV-1 attachment/fusion to cells, protease, integrase, and the nucleocapsid protein. Molecular target-based and cell-based assays...

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