论文信息 - Novel series of [ddN]-[TSAO-T] heterodimers as potential bi-functional inhibitors of HIV-1 RT. Studies in the linker and ddN region. - 字舞流文

Novel series of [ddN]-[TSAO-T] heterodimers as potential bi-functional inhibitors of HIV-1 RT. Studies in the linker and ddN region.

Novel series of [ddN]-(CH2)n-[TSAO-T] heterodimers have been prepared and tested for their anti-HIV-1 and HIV-2 activity. The most active compound of this series was the [d4T]-(CH2)3-[TSAO-T] heterodimer (EC50 = 0.018 +/- 0.03 microM).

E. De Clercq | A. Esteban-Gamboa | J. Balzarini | S. Velázquez | M. Jimeno | M. Pérez-Pérez | C. Chamorro | A. San-Félix | V. Tuñon | M. Camarasa | E. Lobatón

[1] E. De Clercq,et al. Aryl phosphoramidate derivatives of d4T have improved anti-HIV efficacy in tissue culture and may act by the generation of a novel intracellular metabolite. , 1996, Journal of medicinal chemistry.

[2] E. De Clercq,et al. Synthesis and anti-HIV activity of [AZT]-[TSAO-T] and [AZT]-[HEPT] dimers as potential multifunctional inhibitors of HIV-1 reverse transcriptase. , 1995, Journal of medicinal chemistry.

[3] E. De Clercq,et al. Treatment of human immunodeficiency virus type 1 (HIV-1)-infected cells with combinations of HIV-1-specific inhibitors results in a different resistance pattern than does treatment with single-drug therapy , 1993, Journal of virology.

[4] D. Richman,et al. BI-RG-587 is active against zidovudine-resistant human immunodeficiency virus type 1 and synergistic with zidovudine , 1991, Antimicrobial Agents and Chemotherapy.