Purine analogs as CDK enzyme inhibitory agents: a survey and QSAR analysis.
作者： Allen D. Lee , Shijun Ren , Eric J. Lien
DOI: 10.1007/978-3-0348-8319-1_4
关键词: Cell cycle 、 Structure–activity relationship 、 Cyclin-dependent kinase 、 Enzyme inhibitor 、 Purine analogue 、 Cell growth 、 Biology 、 Cyclin-dependent kinase 1 、 Biochemistry 、 Pharmacology 、 Cyclin-dependent kinase 2
摘要: Characterization of the cell cycle has introduced CDKs and other proteins as possible targets for inhibition proliferation, such as, CDK1 CDK2, whose may be useful in treatment proliferative disorders. Structure-activity analyses have been instrumental design discovery potent CDK inhibitors, purine analogs, which increased potency from micromolar to nanomolar level. X-ray crystallography molecular modeling provided evidence that these compounds act on target enzyme. Selected inhibitors successfully entered clinical trials. Further characterization identify inhibit QSAR SAR studies, trials expedite development therapeutic use.
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