Ontology highlight
ABSTRACT:
SUBMITTER: Gladkova ED
PROVIDER: S-EPMC7582571 | biostudies-literature | 2020 Sep
REPOSITORIES: biostudies-literature
Gladkova Elizaveta D ED Nechepurenko Ivan V IV Bredikhin Roman A RA Chepanova Arina A AA Zakharenko Alexandra L AL Luzina Olga A OA Ilina Ekaterina S ES Dyrkheeva Nadezhda S NS Mamontova Evgeniya M EM Anarbaev Rashid O RO Reynisson Jóhannes J Volcho Konstantin P KP Salakhutdinov Nariman F NF Lavrik Olga I OI
International journal of molecular sciences 20200928 19
A series of berberine and tetrahydroberberine sulfonate derivatives were prepared and tested against the tyrosyl-DNA phosphodiesterase 1 (Tdp1) DNA-repair enzyme. The berberine derivatives inhibit the Tdp1 enzyme in the low micromolar range; this is the first reported berberine based Tdp1 inhibitor. A structure-activity relationship analysis revealed the importance of bromine substitution in the 12-position on the tetrahydroberberine scaffold. Furthermore, it was shown that the addition of a sul ...[more]