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Pubmed ID :29329658
Publication Date : //

Novel compounds with potent CDK9 inhibitory activity for the treatment of myeloma.


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).

Authors : Czudor Zsófia , Balogh Mária , Bánhegyi Péter , Boros Sándor , Breza Nóra , Dobos Judit , Fábián Márk , Horváth Zoltán , Illyés Eszter , Markó Péter , Sipos Anna , Szántai-Kis Csaba , Szokol Bálint , Őrfi László ,

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