Synthesis and biological evaluation of selected 7-azaindole derivatives as CDK9/Cyclin T and Haspin inhibitors - CNRS - Centre national de la recherche scientifique Accéder directement au contenu
Article Dans Une Revue Medicinal Chemistry Research Année : 2020

Synthesis and biological evaluation of selected 7-azaindole derivatives as CDK9/Cyclin T and Haspin inhibitors

Résumé

The 7-azaindole scaffold attracts attention due to its value in the design of inhibitors of diseases related protein kinases. However, this scaffold has not been evaluated against Haploid germ cell-specific nuclear protein kinase (Haspin). Herein, we report the synthesis of a select set of 7-azaindole derivatives and their evaluation against Haspin. The compounds were also evaluated against CDK9/Cyclin T kinase. The synthesis of 7-azaindole derivatives was achieved through Suzuki coupling using appropriate halogenated 7-azaindole and boronic acids. Seven of the screened compounds exhibited activity as CDK9/Cyclin T and/or Haspin inhibitors in a nanomolar to low micromolar range. The most promising dual inhibiting compound 18c, exhibited an inhibitory potential of 0.206 µM against CDK9/Cyclin T and 0.118 µM against Haspin. The dual inhibition of CDK9/Cyclin T and Haspin could afford a potentially potent antimitotic agent of value in further anticancer studies.
Fichier non déposé

Dates et versions

hal-03868372 , version 1 (24-11-2022)

Identifiants

Citer

Lianie Pieterse, Lesetja J Legoabe, Richard M Beteck, Béatrice Josselin, Stéphane Bach, et al.. Synthesis and biological evaluation of selected 7-azaindole derivatives as CDK9/Cyclin T and Haspin inhibitors. Medicinal Chemistry Research, 2020, 29, pp.1449 - 1462. ⟨10.1007/s00044-020-02560-1⟩. ⟨hal-03868372⟩
50 Consultations
0 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More