Differential Antiviral Activity of Two TIBO Derivatives Against the Human Immunodeficiency and Murine Leukemia Viruses Alone and in Combination with Other Anti-HIV Agents
作者： ROBERT W. BUCKHEIT , JULIE GERMANY-DECKER , MELINDA G. HOLLINGSHEAD , LOIS B. ALLEN , WILLIAM M. SHANNON
关键词: Viral disease 、 Cell culture 、 Virus 、 Reverse transcriptase 、 Retrovirus 、 Murine leukemia virus 、 Biology 、 Leukemia 、 Virology 、 Cell killing
摘要: R82913 and R86183, two derivatives of tetrahydroimidazo[4,5,1-jk][1,4]-benzodiazepm-2(1H)-thione (TIBO), were found to potently selectively inhibit the replication cell killing effects a panel biologically diverse laboratory clinical strains HIV-1. The compounds exhibited significant activity in all human lines tested, as well fresh peripheral blood lymphocytes macrophages. One these (R82913) was significantly murine retrovirus (Rauscher leukemia virus) both UV-XC plaque formation virus yield reduction assays. despite differing from only positioning single chlorine molecule, not active against but 10-fold more potent inhibiting HIV-1 replication. Combination antiviral assays with other reverse transcriptase inhibitors, including AZT, ddC, carbovir, yielded synergistic anti-HIV TIBO derivatives. Additive slig...
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