2. Academic Validation
  3. 4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6

4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6

  • J Med Chem. 2010 Nov 25;53(22):7938-57. doi: 10.1021/jm100571n.
Young Shin Cho 1,  Maria Borland,  Christopher Brain,  Christine H-T Chen,  Hong Cheng,  Rajiv Chopra,  Kristy Chung,  James Groarke,  Guo He,  Ying Hou,  Sunkyu Kim,  Steven Kovats,  Yipin Lu,  Marc O'Reilly,  Junqing Shen,  Troy Smith,  Gary Trakshel,  Markus Vögtle,  Mei Xu,  Ming Xu,  Moo Je Sung
Affiliations

Affiliation

  • 1 Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, USA. youngshin.cho@novartis
PMID: 21038853 DOI: 10.1021/jm100571n
Abstract

Identification and structure-guided optimization of a series of 4-(pyrazol-4-yl)-pyrimidines as selective CDK4/6 inhibitors is reported herein. Several potency and selectivity determinants were established based on the X-ray crystallographic analysis of representative compounds bound to monomeric CDK6. Significant selectivity for CDK4/6 over CDK1 and CDK2 was demonstrated with several compounds in both enzymatic and cellular assays.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-15612
    CDK
    CDK
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