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

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第一作者： Fleur M,Ferguson

第一单位： Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02215, USA.

作者： Fleur M,Ferguson ^[1] ; Zainab M,Doctor ^[1] ; Scott B,Ficarro ^[2] ; Jarrod A,Marto ^[3] ; Nam Doo,Kim ^[4] ; Taebo,Sim ^[5] ; Nathanael S,Gray ^[6]

作者单位： Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02215, USA. ^[1] Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Blais Proteomics Center, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Pathology, Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02215, USA. ^[2] Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Blais Proteomics Center, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Pathology, Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02215, USA; Department of Oncologic Pathology, Dana-Farber Cancer Institute, Boston, MA 02215, USA. ^[3] Daegu-Gyeongbuk Medical Innovation Foundation, Republic of Korea. ^[4] Chemical Kinomics Research Center, Korea Institute of Science and Technology, Republic of Korea; KU-KIST Graduate School of Converging Science and Technology, Korea University, Republic of Korea. ^[5] Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA. Electronic address: nathanael_gray@dfci.harvard.edu. ^[6]

关键词 CDK inhibitor CDK14 CDK15 CDK16 CDK17 CDK18 Cell cycle Covalent kinase inhibitor Mitosis TAIRE kinase

主题词细胞周期蛋白质依赖激酶类(Cyclin-Dependent Kinases);人类(Humans);蛋白激酶抑制剂(Protein Kinase Inhibitors);吡唑类(Pyrazoles);构效关系(Structure-Activity Relationship)

DOI 10.1016/j.bmcl.2019.05.024

PMID 31175010

发布时间 2020-09-09

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