title: Discovery of a novel class of 2-aminopyrimidines as CDK1 and CDK2 inhibitors.
abstract: A series of new 2-(2-aminopyrimidin-4-yl)phenol derivatives were synthesized as potential antitumor compounds. Substitution with pyrrolidine-3,4-diol at the 4-position of phenol provided potent inhibitory activity against CDK1 and CDK2. X-ray crystal structural studies were performed to account for the effect of the substituent on both the enzymatic and cell growth inhibitory activities.
authors.affiliation: Department of Chemistry, Keimyung University, Daegu 704-701, South Korea. jinho@kmu.ac.kr
authors.forename: Jinho
authors.initials: J
authors.lastname: Lee
authors.forename: Kyoung-Hee
authors.initials: KH
authors.lastname: Kim
authors.forename: Shinwu
authors.initials: S
authors.lastname: Jeong
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D001665:Binding Sites; D016203:CDC2 Protein Kinase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D045744:Cell Line, Tumor; D003198:Computer Simulation; D051357:Cyclin-Dependent Kinase 2 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; C012180:2-aminopyrimidine; D016203:CDC2 Protein Kinase; D051357:Cyclin-Dependent Kinase 2