期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 17, 期 23, 页码 7850-7860出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.10.039
关键词
Cyclin D1/CDK4 inhibitor; Thieno[2,3-d]pyrimidin-4-yl hydrazone
The design, synthesis and evaluation of novel thieno[2,3-d]pyrimidin-4-yl hydrazone analogues as cyclin-dependent kinase 4 (CDK4) inhibitor are described. Focusing on the optimization of the heteroaryl moiety at the hydrazone with substituted phenyl groups, 4-[(methylamino)methyl]benzaldehyde (22) and 5-iso-indolinecarbaldehyde (24) (6-tert-butylthieno[2,3-d]pyrimidin-4-yl) hydrazone derivatives have been identified. In this paper, the potency, selectivity profile and structure-activity relationships of our synthetic compounds are discussed. (c) 2009 Elsevier Ltd. All rights reserved.
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