| Literature DB >> 29329658 |
Zsófia Czudor1, Mária Balogh2, Péter Bánhegyi2, Sándor Boros2, Nóra Breza2, Judit Dobos2, Márk Fábián1, Zoltán Horváth2, Eszter Illyés2, Péter Markó2, Anna Sipos2, Csaba Szántai-Kis2, Bálint Szokol2, László Őrfi3.
Abstract
Cyclin-dependent kinases (CDKs) and Polo-like kinases (PLKs) play key role in the regulation of the cell cycle. The aim of our study was originally the further development of our recently discovered polo-like kinase 1 (PLK1) inhibitors. A series of new 2,4-disubstituted pyrimidine derivatives were synthesized around the original hit, but their PLK1 inhibitory activity was very poor. However the novel compounds showed nanomolar CDK9 inhibitory activity and very good antiproliferative effect on multiple myeloma cell lines (RPMI-8226).Entities:
Keywords: 2,4-Disubstituted pyrimidine; Cyclin dependent kinase inhibitor; Multiple myeloma; Polo-like kinase
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Year: 2018 PMID： 29329658 DOI： 10.1016/j.bmcl.2018.01.002
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823