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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  • Horiuchi Takao
    Lead Discovery & Optimization Research Laboratories II, Daiichi Sankyo Co., Ltd.
  • Takeda Yasuyuki
    Lead Discovery & Optimization Research Laboratories II, Daiichi Sankyo Co., Ltd.
  • Haginoya Noriyasu
    Lead Discovery & Optimization Research Laboratories II, Daiichi Sankyo Co., Ltd.
  • Miyazaki Masaki
    Lead Discovery & Optimization Research Laboratories II, Daiichi Sankyo Co., Ltd.
  • Nagata Motoko
    Oncology Research Laboratories, Daiichi Sankyo Co., Ltd.
  • Kitagawa Mayumi
    Oncology Research Laboratories, Daiichi Sankyo Co., Ltd.
  • Akahane Kouichi
    Oncology Research Laboratories, Daiichi Sankyo Co., Ltd.
  • Uoto Kouichi
    Lead Discovery & Optimization Research Laboratories II, Daiichi Sankyo Co., Ltd.

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  • 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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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.

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