2. Academic Validation
  3. Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases

Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases

  • Bioorg Med Chem Lett. 2004 Jun 7;14(11):2973-7. doi: 10.1016/j.bmcl.2004.02.105.
Raj N Misra 1,  Hai-yun Xiao,  David K Williams,  Kyoung S Kim,  Songfeng Lu,  Kristen A Keller,  Janet G Mulheron,  Roberta Batorsky,  John S Tokarski,  John S Sack,  S David Kimball,  Francis Y Lee,  Kevin R Webster
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. raj_n_misra@hotmail.com
PMID: 15125971 DOI: 10.1016/j.bmcl.2004.02.105
Abstract

N-Aryl aminothiazoles 6-9 were prepared from 2-bromothiazole 5 and found to be CDK inhibitors. In cells they act as potent cytotoxic agents. Selectivity for CDK1, CDK2, and CDK4 was dependent of the nature of the N-aryl group and distinct from the CDK2 selective N-acyl analogues. The N-2-pyridyl analogues 7 and 19 showed pan CDK inhibitory activity. Elaborated analogues 19 and 23 exhibited Anticancer activity in mice against P388 murine leukemia. The solid-state structure of 7 bound to CDK2 shows a similar binding mode to the N-acyl analogues.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-182734
    CDK抑制剂
    CDK
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