Qhobosheane, Malikotsi A.Legoabe, Lesetja J.Petzer, Jacobus P.Beteck, Richard M.Josselin, Béatrice2020-04-202020-04-202020Qhobosheane, M.A. et al. 2020. Synthesis and evaluation of 7-azaindole derivatives bearing benzocycloalkanone motifs as protein kinase inhibitors. Bioorganic and medicinal chemistry, #115468. [https://doi.org/10.1016/j.bmc.2020.115468]0968-0896http://hdl.handle.net/10394/34563https://www.sciencedirect.com/science/article/pii/S0968089620302820https://doi.org/10.1016/j.bmc.2020.115468Protein kinases are important drug targets, especially in the area of oncology. This paper reports the synthesis and biological evaluation of new 7-azaindole derivatives bearing benzocycloalkanone motifs as potential protein kinase inhibitors. Four compounds 8g, 8h, 8i, and 8l were discovered to inhibit cyclin-dependent kinase 9 (CDK9/CyclinT) and/or Haspin kinase in the micromolar to nanomolar range. 8l was identified as the most potent Haspin inhibitor (IC50 = 14 nM), while 8g and 8h acted as dual inhibitors of CDK9/CyclinT and Haspin. These novel compounds constitute a promising starting point for the discovery of dual protein kinase inhibitors that have potential to be developed as anticancer agents, since both CDK9/CyclinT and Haspin are considered to be drug targets in oncologyen7-AzaindoleBenzocycloalkanoneProtein kinaseStructure-activity relationshipHaspinCDK9/CyclinTDual inhibitorOncologyArticle