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- W1985243721 abstract "A novel series of benzophenone derivatives with B-ring substituted by naphthyl ring has been synthesized and evaluated as non-nucleoside HIV-1 reverse transcriptase inhibitors. Most of these compounds showed good to moderate activity against wild-type HIV-1 and mutated viruses. In particular, the analogue 10i demonstrated the most potent activity against wild-type HIV-1 with an EC₅₀ value of 4.8 nM, and with a high selectivity index up to 10347.9, it also proved to be active against the HIV-1 double mutant strain A₁₇ (K103N+Y181C) with an EC₅₀ value of 2.1 μM. In addition, the molecular modeling study was used to explore the major interactions between the potent inhibitors with the HIV-1 RT. The investigation of the structure-activity relationships may serve as an important lead for the further optimization." @default.
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- W1985243721 date "2011-08-01" @default.
- W1985243721 modified "2023-09-23" @default.
- W1985243721 title "Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors" @default.
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- W1985243721 doi "https://doi.org/10.1016/j.bmc.2011.06.007" @default.
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