Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14

Bioorg Med Chem Lett. 2019 Aug 1;29(15):1985-1993. doi: 10.1016/j.bmcl.2019.05.024. Epub 2019 May 23.


The TAIRE family of kinases are an understudied branch of the CDK kinase family, that have been implicated in a number of cancers. This manuscript describes the design, synthesis and SAR of covalent CDK14 inhibitors, culminating in identification of FMF-04-159-2, a potent, covalent CDK14 inhibitor with a TAIRE kinase biased selectivity profile.

Keywords: CDK inhibitor; CDK14; CDK15; CDK16; CDK17; CDK18; Cell cycle; Covalent kinase inhibitor; Mitosis; TAIRE kinase.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyclin-Dependent Kinases / pharmacology
  • Cyclin-Dependent Kinases / therapeutic use*
  • Humans
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use*
  • Pyrazoles / chemistry*
  • Structure-Activity Relationship


  • Protein Kinase Inhibitors
  • Pyrazoles
  • CDK14 protein, human
  • Cyclin-Dependent Kinases