Azido-containing aryl beta-diketo acid HIV-1 integrase inhibitors |
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Authors: | Zhang Xuechun Pais Godwin C G Svarovskaia Evguenia S Marchand Christophe Johnson Allison A Karki Rajeshri G Nicklaus Marc C Pathak Vinay K Pommier Yves Burke Terrence R |
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Affiliation: | Laboratory of Medicinal Chemistry, Center for Cancer Research, National Cancer Institute, National Institutes of Health, MD, USA. |
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Abstract: | Aryl beta-diketo acids (ADK) comprise a general class of potent HIV-1 integrase (IN) inhibitors, which can exhibit selective inhibition of strand transfer reactions in extracellular recombinant IN assays and provide potent antiviral effects in HIV-infected cells. Recent studies have shown that polycyclic aryl or aryl rings bearing aryl-containing substituents are components of potent members of this class. Reported herein is the first use of azido functionality as an aryl replacement in beta-diketo acid IN inhibitors. The ability of azido-containing inhibitors to exhibit potent inhibition of IN and antiviral protection in HIV-infected cells, renders the azide group of potential value in the further development of ADK-based IN inhibitors. |
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