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. 1990 Dec 7;250(4986):1411-3.
doi: 10.1126/science.1701568.

Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor

V J Merluzzi  1 , K D Hargrave, M Labadia, K Grozinger, M Skoog, J C Wu, C K Shih, K Eckner, S Hattox, J Adams, et al.
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Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor

V J Merluzzi et al. Science. .

Erratum in

  • Science 1991 Jan 25;251(4992):362

Abstract

A series of dipyridodiazepinones have been shown to be potent inhibitors of human immunodeficiency virus-1 (HIV-1) reverse transcriptase (RT). One compound, BI-RG-587, had a Ki of 200 nanomolar for inhibition of HIV-1 RT that was noncompetitive with respect to deoxyguanosine triphosphate. BI-RG-587 was specific for HIV-1 RT, having no effect on feline and simian RT or any mammalian DNA polymerases. BI-RG-587 inhibited HIV-1 replication in vitro as demonstrated by in situ hybridization, inhibition of protein p24 production, and the lack of syncytia formation in cultured human T cell lines and freshly isolated human peripheral blood lymphocytes. Cytotoxicity studies of BI-RG-587 on human cells showed a high therapeutic index (greater than 8000) in culture.

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