Discovery of Novel Thieno[2,3-d]pyrimidin-4-yl Hydrazone-Based Cyclin-Dependent Kinase 4 Inhibitors: Synthesis, Biological Evaluation and Structure-Activity Relationships

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Abstract

The design, synthesis, and evaluation of novel thieno[2,3-d]pyrimidin-4-yl hydrazone analogues as cyclin-dependent kinase 4 (CDK4) inhibitors are described. In continuing our program aim to search for potent CDK4 inhibitors, the introduction of a thiazole group at the hydrazone part has led to marked enhancement of chemical stability. Furthermore, by focusing on the optimization at the C-4′ position of the thiazole ring and the C-6 position of the thieno[2,3-d]pyrimidine moiety, compound 35 has been identified with efficacy in a xenograft model of HCT116 cells. In this paper, the potency, selectivity profile, and structure–activity relationships of our synthetic compounds are discussed.

Journal

Pharmaceutical Bulletin  

Pharmaceutical Bulletin 59(8), 991-1002, 2011 

The Pharmaceutical Society of Japan

Codes

  • NII Article ID (NAID) :
    130000960931
  • NII NACSIS-CAT ID (NCID) :
    AA00602100
  • Text Lang :
    EN
  • ISSN :
    0009-2363
  • NDL Article ID :
    11174305
  • NDL Source Classification :
    ZS51(科学技術--薬学) // ZP1(科学技術--化学・化学工業)
  • NDL Call No. :
    Z53-D167
  • Data Source :
    NDL  J-STAGE