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Note | Regular issue | Vol 45, No. 11, 1997, pp.2277-2282
Published online, 1st January, 1970
DOI: 10.3987/COM-97-7952
Design and Synthesis of Photoactivatable Coumarin-containing HIV-1 Integrase Inhibitors

He Zhao, Nouri Neamati, Yves Pommier, and Terrence R. Burke, Jr.*

*Laboratories of Medicinal Chemistry, Division of Basic Sciences, National Cancer Institute, Building 37, Room 5C06, National Institute of Health, Bethesda, MD 20892, U.S.A.


Three dimeric coumarin analogues (1 - 3) were prepared, each containing the photoactivatable benzophenone moiety. These compounds exhibited low micromolar IC50 values against HIV-1 integrase mediated 3’-processing and strand transfer, and may represent useful probes for elucidating enzyme-inhibitor interactions.