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Synthesis of nucleoside 5′-O-α,β-methylene-β-triphosphates and evaluation of their potency towards inhibition of HIV-1 reverse transcriptase

Year: 2010

Type: article

Abstract: A polymer-bound alpha,beta-methylene-beta-triphosphitylating reagent was synthesized and subjected to reactions with unprotected nucleosides, followed by oxidation, deprotection of cyanoethoxy groups, and acidic cleavage to afford nucleoside 5'-O-alpha,beta-methylene-beta-triphosphates. Among all the compounds, cytidine 5'-O-alpha,beta-methylene-beta-triphosphate inhibited RNase H activity of HIV-1 reverse transcriptase with a K(i) value of 225 microM.

Source: Organic & Biomolecular Chemistry

DOI: 10.1039/b922846b

Authors: Y. Ahmadibeni, C. Dash, M. J. Hanley, S. F. J. Le Grice, H. K. Agarwal, K. Parang

Institutions: University of Rhode Island, Columbus State University, Meharry Medical College, National Institutes of Health, Frederick National Laboratory for Cancer Research, National Cancer Institute

Language: English

Topic: HIV/AIDS drug development and treatment

Subfield: Infectious Diseases

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: green

Funders: National Science Foundation, National Institutes of Health, National Institute on Drug Abuse, National Cancer Institute, National Center for Research Resources, National Institute on Minority Health and Health Disparities

Awards: Role of nucleic acid structure in HIV-1 replication, Cocaine downregulates anti-HIV microRNAs in CD4+ T cells, G2099372222, Meharry Clinical and Translational Research Center (MeTRC), Meharry Clinical and Translational Research Center (MeTRC), Small molecule targeting viral nucleotidyltransferases, Cocaine-Induced Epigenetic Changes in CD4+ T cells and HIV-1 Replication

OpenAlex ID: W2053838970

FWCI: 0.83

Cites: 35

Cited by: 8

Related to: 10