dc.contributor.author | Qhobosheane, Malikotsi A. | |
dc.contributor.author | Legoabe, Lesetja J. | |
dc.contributor.author | Petzer, Jacobus P. | |
dc.contributor.author | Beteck, Richard M. | |
dc.contributor.author | Josselin, Béatrice | |
dc.date.accessioned | 2020-04-20T07:50:24Z | |
dc.date.available | 2020-04-20T07:50:24Z | |
dc.date.issued | 2020 | |
dc.identifier.citation | Qhobosheane, 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] | en_US |
dc.identifier.issn | 0968-0896 | |
dc.identifier.uri | http://hdl.handle.net/10394/34563 | |
dc.identifier.uri | https://www.sciencedirect.com/science/article/pii/S0968089620302820 | |
dc.identifier.uri | https://doi.org/10.1016/j.bmc.2020.115468 | |
dc.description.abstract | Protein 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 oncology | en_US |
dc.language.iso | en | en_US |
dc.publisher | Elsevier | en_US |
dc.subject | 7-Azaindole | en_US |
dc.subject | Benzocycloalkanone | en_US |
dc.subject | Protein kinase | en_US |
dc.subject | Structure-activity relationship | en_US |
dc.subject | Haspin | en_US |
dc.subject | CDK9/CyclinT | en_US |
dc.subject | Dual inhibitor | en_US |
dc.subject | Oncology | en_US |
dc.title | Synthesis and evaluation of 7-azaindole derivatives bearing benzocycloalkanone motifs as protein kinase inhibitors | en_US |
dc.type | Article | en_US |
dc.contributor.researchID | 10727388 - Petzer, Jacobus Petrus | |
dc.contributor.researchID | 12902608 - Legoabe, Lesetja Jan | |
dc.contributor.researchID | 25159194 - Beteck, Richard Mbi | |
dc.contributor.researchID | 27836576 - Qhobosheane, Malikotsi A. | |