Synthesis of Mimics to 5-(2″-thienyl)-2′,3′-β-Dideoxyuridine Triphosphate
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Hiv Rt
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A series of 5′-amido derivatives of 5-(2″-thienyl)-2′,3′,5′-β-trideoxyuridine were prepared. The compounds were tested for their inhibition of cellular DNA polymerase α and α HIV-RT. The succinic fumaric and maleic acid derivatives of 5-(2″-thienyl)-2′,3′,5′-β-trideoxyuridine were investigated. None of the compounds inhibited HIV-RT. The fumaric acid derivative inhibited DNA pol α with IC50 33 μg ml−1. The succinic acid derivative was about half as active with IC50 76 μg ml−1. The 5′-N-acyl derivatives also were structurally compared to the monomethyl ester of the triphosphate using the Sybyl program.
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2011 ◽
Vol 239-242
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pp. 219-222
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1960 ◽
Vol 04
(03)
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pp. 462-472
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2018 ◽
Vol 14
(65)
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pp. 028
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1956 ◽
Vol 21
(6)
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pp. 1500-1512
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1965 ◽
Vol 30
(4)
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pp. 940-951
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1969 ◽
Vol 34
(11)
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pp. 3325-3335
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