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• W2005210168 abstract "Out of a series of eight new phosphonate nucleosides with an l-threose and an l-2-deoxythreose sugar moiety, two new compounds were identified (PMDTA and PMDTT) that showed potent anti-HIV-1 (HIV-2) activity [EC50 = 2.53 microM (PMDTA) and 6.59 microM (PMDTT)], while no cytoxicity was observed at the highest concentration tested [CC50 > 316 microM (PMDTA) and > 343 microM (PMDTT)]. The kinetics of incorporation of PMDTA into DNA (using the diphosphate of PMDTA as substrate and HIV-1 reverse transcriptase as catalyst) was similar to the kinetics observed for dATP, while the diphosphate of PMDTA was a very poor substrate for DNA polymerase alpha. The incorporated PMDTA fits very well in the active site pocket of HIV-1 reverse transcriptase." @default.
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• W2005210168 date "2005-03-19" @default.
• W2005210168 modified "2023-09-30" @default.
• W2005210168 title "Deoxythreosyl Phosphonate Nucleosides as Selective Anti-HIV Agents" @default.
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• W2005210168 doi "https://doi.org/10.1021/ja043045z" @default.
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