Comparison of the effect of Carbovir, AZT, and dideoxynucleoside triphosphates on the activity of human immunodeficiency virus reverse transcriptase and selected human polymerases.
E L White, W B Parker, L J Macy, S C Shaddix, G McCaleb, J A Secrist, R Vince, W M Shannon
Index: Biochem. Biophys. Res. Commun. 161 , 393, (1989)
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Abstract
Carbocylic 2',3'-didehydro-2',3'-dideoxyguanosine (Carbovir; NSC 614846) is an antiretroviral agent which may be useful in the treatment of AIDS. We have synthesized the 5'-triphosphate of Carbovir and examined its ability to inhibit human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (EC 2.7.7.49) and other retroviral reverse transcriptases, as well as human DNA polymerases alpha, beta, gamma (EC 2.7.7.7) and DNA primase (EC 2.7.7.6). Carbovir triphosphate emerges as a highly selective inhibitor of reverse transcriptases with little, if any, effect on the cellular enzymes. 3'-Azido-2',3'-dideoxythymidine (AZT) triphosphate and the two dideoxynucleoside triphosphates, ddTTP and ddGTP, inhibited HIV-1 reverse transcriptase to the same degree as Carbovir triphosphate, but were less selective in that they also inhibited DNA polymerases beta and gamma. We conclude that Carbovir is a highly selective antiretroviral agent.
Related Compounds
| Structure | Name/CAS No. | Molecular Formula | Articles |
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![(1S)-(+)-2-Azabicyclo[2.2.1]hept-5-en-3-one Structure](https://image.chemsrc.com/caspic/022/130931-83-8.png) |
(1S)-(+)-2-Azabicyclo[2.2.1]hept-5-en-3-one
CAS:130931-83-8 |
C6H7NO |
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Synthesis and anti-HIV activity of carbocyclic 2',3'-didehyd...
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