Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 199, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112355
Keywords
Kinases; CDK9; CDK10; Cytotoxicity; Kinase inhibitors; Structure-activity relationship
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Funding
- CNRS
- University Paris-Saclay throughout an Equipe Labellisee 2014 grant
- La Ligue Contre le Cancer throughout an Equipe Labellisee 2014 grant
- La Ligue contre le Cancer Grand Ouest
- [ANR-10-LABX-33]
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In this work, unique flavopiridol analogs bearing thiosugars, amino acids and heterocyclic moieties tethered to the flavopiridol via thioether and amine bonds mainly on its C ring have been prepared. The analogs bearing thioether-benzimidazoles as substituents have demonstrated high cytotoxic activity in vitro against up to seven cancer cell lines. Their cytotoxic effects are comparable to those of flavopiridol. The most active compound 13c resulting from a structure-activity relationship (SAR) study and in silico docking showed the best antiproliferative activity and was more efficient than the reference compound. In addition, compound 13c showed significant nanomolar inhibition against CDK9, CDK10, and GSK3 beta protein kinases. (C) 2020 Elsevier Masson SAS. All rights reserved.
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