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

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

Research output: Contribution to journalArticle

2 Citations (Scopus)

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).

Original languageEnglish
Pages (from-to)769-773
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume28
Issue number4
DOIs
Publication statusPublished - Feb 15 2018

Fingerprint

Cells
Cyclin-Dependent Kinases
Multiple Myeloma
Cell Cycle
Phosphotransferases
Derivatives
Cell Line
polo-like kinase 1
pyrimidine

Keywords

  • 2,4-Disubstituted pyrimidine
  • Cyclin dependent kinase inhibitor
  • Multiple myeloma
  • Polo-like kinase

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Novel compounds with potent CDK9 inhibitory activity for the treatment of myeloma. / Czudor, Zsófia; Balogh, Mária; Bánhegyi, Péter; Boros, Sándor; Breza, Nóra; Dobos, J.; Fábián, Márk; Horváth, Zoltán; Illyés, Eszter; Markó, Péter; Sipos, Anna; Szántai-Kis, Csaba; Szokol, Bálint; Őrfi, L.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 28, No. 4, 15.02.2018, p. 769-773.

Research output: Contribution to journalArticle

Czudor, Z, Balogh, M, Bánhegyi, P, Boros, S, Breza, N, Dobos, J, Fábián, M, Horváth, Z, Illyés, E, Markó, P, Sipos, A, Szántai-Kis, C, Szokol, B & Őrfi, L 2018, 'Novel compounds with potent CDK9 inhibitory activity for the treatment of myeloma', Bioorganic and Medicinal Chemistry Letters, vol. 28, no. 4, pp. 769-773. https://doi.org/10.1016/j.bmcl.2018.01.002
Czudor, Zsófia ; Balogh, Mária ; Bánhegyi, Péter ; Boros, Sándor ; Breza, Nóra ; Dobos, J. ; Fábián, Márk ; Horváth, Zoltán ; Illyés, Eszter ; Markó, Péter ; Sipos, Anna ; Szántai-Kis, Csaba ; Szokol, Bálint ; Őrfi, L. / Novel compounds with potent CDK9 inhibitory activity for the treatment of myeloma. In: Bioorganic and Medicinal Chemistry Letters. 2018 ; Vol. 28, No. 4. pp. 769-773.
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