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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.
V J Merluzzi, and
K D Hargrave, and
M Labadia, and
K Grozinger, and
M Skoog, and
J C Wu, and
C K Shih, and
K Eckner, and
S Hattox, and
J Adams
October 2004,
Current HIV research,
V J Merluzzi, and
K D Hargrave, and
M Labadia, and
K Grozinger, and
M Skoog, and
J C Wu, and
C K Shih, and
K Eckner, and
S Hattox, and
J Adams
February 1995,
Science (New York, N.Y.),
V J Merluzzi, and
K D Hargrave, and
M Labadia, and
K Grozinger, and
M Skoog, and
J C Wu, and
C K Shih, and
K Eckner, and
S Hattox, and
J Adams
August 2019,
Antimicrobial agents and chemotherapy,
V J Merluzzi, and
K D Hargrave, and
M Labadia, and
K Grozinger, and
M Skoog, and
J C Wu, and
C K Shih, and
K Eckner, and
S Hattox, and
J Adams
October 2000,
AIDS research and human retroviruses,
V J Merluzzi, and
K D Hargrave, and
M Labadia, and
K Grozinger, and
M Skoog, and
J C Wu, and
C K Shih, and
K Eckner, and
S Hattox, and
J Adams
June 1997,
Nature medicine,
V J Merluzzi, and
K D Hargrave, and
M Labadia, and
K Grozinger, and
M Skoog, and
J C Wu, and
C K Shih, and
K Eckner, and
S Hattox, and
J Adams
May 1996,
Biochemical Society transactions,
V J Merluzzi, and
K D Hargrave, and
M Labadia, and
K Grozinger, and
M Skoog, and
J C Wu, and
C K Shih, and
K Eckner, and
S Hattox, and
J Adams
January 1996,
Biochemistry,
V J Merluzzi, and
K D Hargrave, and
M Labadia, and
K Grozinger, and
M Skoog, and
J C Wu, and
C K Shih, and
K Eckner, and
S Hattox, and
J Adams
December 2004,
Antimicrobial agents and chemotherapy,
V J Merluzzi, and
K D Hargrave, and
M Labadia, and
K Grozinger, and
M Skoog, and
J C Wu, and
C K Shih, and
K Eckner, and
S Hattox, and
J Adams
June 1997,
Biochemistry,
V J Merluzzi, and
K D Hargrave, and
M Labadia, and
K Grozinger, and
M Skoog, and
J C Wu, and
C K Shih, and
K Eckner, and
S Hattox, and
J Adams
January 2014,
Antimicrobial agents and chemotherapy,
