4'-Ethynyl-2'-deoxyadenosine (4'-E-dA) is a nucleoside reversetranscriptase (RT) inhibitor. It is potent against drug-resistant HIV variants (EC50: 98 nM in MT-4 cells for anti-HIV-1 activity).
Loviride is a non-nucleoside reversetranscriptaseinhibitor (IC50: 0.3 µM). Loviride inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells. It is used for reversetranscriptase from HIV-1.
(+)-Carbovir triphosphate is an active metabolite of Abacavir. It was used to study the molecular mechanism of inhibition and drug resistance for HIV-1 reversetranscriptase.
Stampidine can prevent the sexual transmission of HIV-1. It exhibited remarkable subnanomolar to low nanomolar in vitro antiretroviral potency against nucleoside reversetranscriptaseinhibitor-resistant primary clinical HIV isolates, non-nucleoside RT-re
AIC-292 is a potent reversetranscriptaseinhibitor with well tolerated in different cell lines. In addition, activity of AIC292 could be demonstrated against a broad panel of wild-type HIV-1 group. AIC292 also retained activity against viruses harboring
GSK 224876 is a novel next-generation nonnucleoside reversetranscriptaseinhibitor (NNRTI). It has activity against efavirenz-resistant strains in the treatment of treatment-naive HIV-1-infected subjects.
L-696229 is a specific inhibitor of human immunodeficiency virus type 1 (HIV-1) reversetranscriptase (RT). L-696229 inhibited RT activity in a mutually exclusive manner with respect to either phosphonoformate or azidothymidine triphosphate and was a weak
R-82913 is a RNA-directed DNA polymerase inhibitor. R 82913 reduce 5-HT2 receptor-mediated DOI-head-shakes in mice. R82913 inhibited the replication of thirteen different strains of HIV-1 in CEM cells with a median IC50 of 0.15 microM. R82913 was 20-fold
SM111 inhibits in vitro replication of HIV-1, including strains resistant to reversetranscriptase, licensed protease, and integrase inhibitors, without major cellular toxicity.
β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycininhibits HIV-1 reversetranscriptase activity by 39.7% when used at a concentration of 10 μM. It also has antibacterial activity against Gram-positive bacteria. The structure of β-rubromycin was originally described as containing an ortho-quinone group, but it was revised to a para-quinone group in 2000 using organic and biosynthetic methods, as well as spectroscopic analysis.1,2,3References1. Ueno, T., Takahashi, H., Oda, M., et al. Inhibition of human telomerase by rubromycins: Implication of spiroketal system of the compounds as an active moiety. Biochemistry 39(20), 5995-6002 (2000).2. Puder, C., Loya, S., Hizi, A., et al. Structural and biosynthetic investigations of the rubromycins. Eur. J. Org. Chem. 2000(5), 729-735 (2000).3. Goldman, M.E., Salituro, G.S., Bowen, J.A., et al. Inhibition of human immunodeficiency virus-1 reversetranscriptase activity by rubromycins: Competitive interaction at the template.primer site. Mol. Pharmacol. 38(1), 20-25 (1990). β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycininhibits HIV-1 reversetranscriptase activity by 39.7% when used at a concentration of 10 μM. It also has antibacterial activity against Gram-positive bacteria. The structure of β-rubromycin was originally described as containing an ortho-quinone group, but it was revised to a para-quinone group in 2000 using organic and biosynthetic methods, as well as spectroscopic analysis.1,2,3 References1. Ueno, T., Takahashi, H., Oda, M., et al. Inhibition of human telomerase by rubromycins: Implication of spiroketal system of the compounds as an active moiety. Biochemistry 39(20), 5995-6002 (2000).2. Puder, C., Loya, S., Hizi, A., et al. Structural and biosynthetic investigations of the rubromycins. Eur. J. Org. Chem. 2000(5), 729-735 (2000).3. Goldman, M.E., Salituro, G.S., Bowen, J.A., et al. Inhibition of human immunodeficiency virus-1 reversetranscriptase activity by rubromycins: Competitive interaction at the template.primer site. Mol. Pharmacol. 38(1), 20-25 (1990).