dc.contributor.author | Pieterse, Lianie | |
dc.contributor.author | Legoabe, Lesetja J. | |
dc.contributor.author | Beteck, Richard M. | |
dc.contributor.author | Josselin, Béatrice | |
dc.contributor.author | Bach, Stéphane | |
dc.date.accessioned | 2020-06-04T10:35:35Z | |
dc.date.available | 2020-06-04T10:35:35Z | |
dc.date.issued | 2020 | |
dc.identifier.citation | Pieterse, L. et al. 2020. Synthesis and biological evaluation of selected 7-azaindole derivatives as CDK9/Cyclin T and Haspin inhibitors. Medicinal chemistry research, 29:1449-1462. [https://doi.org/10.1007/s00044-020-02560-1] | en_US |
dc.identifier.issn | 1054-2523 | |
dc.identifier.issn | 1554-8120 (Online) | |
dc.identifier.uri | http://hdl.handle.net/10394/34737 | |
dc.identifier.uri | https://link.springer.com/article/10.1007/s00044-020-02560-1 | |
dc.identifier.uri | https://doi.org/10.1007/s00044-020-02560-1 | |
dc.description.abstract | 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 | en_US |
dc.language.iso | en | en_US |
dc.publisher | Springer | en_US |
dc.subject | Protein kinases | en_US |
dc.subject | 7-Azaindole | en_US |
dc.subject | Anticancer | en_US |
dc.subject | CDK9/ Cyclin T | en_US |
dc.subject | Haspin | en_US |
dc.title | Synthesis and biological evaluation of selected 7-azaindole derivatives as CDK9/Cyclin T and Haspin inhibitors | en_US |
dc.type | Article | en_US |
dc.contributor.researchID | 12902608 - Legoabe, Lesetja Jan | |
dc.contributor.researchID | 25159194 - Beteck, Richard Mbi | |
dc.contributor.researchID | 23347368 - Pieterse, Lianie | |