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  • Title: Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.
    Author: Liang YH, He QQ, Zeng ZS, Liu ZQ, Feng XQ, Chen FE, Balzarini J, Pannecouque C, Clercq ED.
    Journal: Bioorg Med Chem; 2010 Jul 01; 18(13):4601-5. PubMed ID: 20570527.
    Abstract:
    Nine newly 6-cyano-2-naphthyl substituted diarylpyrimidines (DAPY) were synthesized as non-nucleoside reverse transcriptase inhibitors on the basis of our previous work. The antiviral and cytotoxicity evaluation indicated that these compounds displayed strong activity against wild-type HIV-1 at nanomolar concentrations with selectivity index SI greater than 23 779. The most active compounds 3c and 3e exhibited activity against the double mutant (103N+181C) strains at an EC₅₀ of 0.16 and 0.15 μM, and were more activity than that of efavirenz.
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