Inhibition of human DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 (Tdp1) by different chiral lipophilic nucleoside derivatives was studied. New Tdp1 inhibitors were found in the series of the studied compounds… Click to show full abstract
Inhibition of human DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 (Tdp1) by different chiral lipophilic nucleoside derivatives was studied. New Tdp1 inhibitors were found in the series of the studied compounds with IC50 = 2.7–6.7 μM. It was shown that D-lipophilic nucleoside derivatives manifested higher inhibition activity than their L-analogs, and configuration of the carbohydrate moiety can influence the mechanism of Tdp1 inhibition.
Keywords:
inhibition;
phosphodiesterase tdp1;
dna phosphodiesterase;
stereochemistry;
tyrosyl dna
Journal Title: Molecules
Year Published: 2022
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Journal Title: Molecules
Year Published: 2022
Link to full text (if available)
Share on Social Media: Sign Up to like & get
recommendations!