Benzophenone Derivatives: a Novel Scaffold as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors

Developing non-nucleoside HIV-1 reverse transcriptase inhibitors (NNRTIs) with improved drug resistance profiles is still a great challenge owing to the rapid emergence of resistant virus. For the potential activity against both wild-type and clinically relevant NNRTI-resistant mutant HIV-1 strains, the novel NNRTI benzophenone derivatives (BPs) have drawn great attention. Considerable efforts on modifying this template have led to the identification of the most active BP analogue, GW678248, which has been progressed to the phase II clinical studies owing to its high anti-HIV-1 activity, low clearance and stable metabolic property. Therefore, this review focused on the benzophenone deravitives provided valuable SAR information for further modifying this scaffold.