title: The design and synthesis of purine inhibitors of CDK2. III.
abstract: Cyclin-dependent kinases (CDKs) belong to a class of enzymes that control the ability of a cell to enter into and proceed through the cell division cycle. Using purine as a scaffold, we have synthesized a number of nanomolar inhibitors of CDK-2/cyclin E. In this report, the synthesis of a series of piperidine-substituted purine analogs will be presented, as well as some of their in vitro and in vivo biological effects.
authors.affiliation: Aventis Pharmaceuticals Inc., Rt. 202-206, Bridgewater, New Jersey 08807, USA.
authors.forename: P W
authors.initials: PW
authors.lastname: Shum
authors.forename: N P
authors.initials: NP
authors.lastname: Peet
authors.forename: P M
authors.initials: PM
authors.lastname: Weintraub
authors.forename: T B
authors.initials: TB
authors.lastname: Le
authors.forename: Z
authors.initials: Z
authors.lastname: Zhao
authors.forename: F
authors.initials: F
authors.lastname: Barbone
authors.forename: B
authors.initials: B
authors.lastname: Cashman
authors.forename: J
authors.initials: J
authors.lastname: Tsay
authors.forename: S
authors.initials: S
authors.lastname: Dwyer
authors.forename: P C
authors.initials: PC
authors.lastname: Loos
authors.forename: E A
authors.initials: EA
authors.lastname: Powers
authors.forename: K
authors.initials: K
authors.lastname: Kropp
authors.forename: P S
authors.initials: PS
authors.lastname: Wright
authors.forename: A
authors.initials: A
authors.lastname: Bitonti
authors.forename: J
authors.initials: J
authors.lastname: Dumont
authors.forename: D R
authors.initials: DR
authors.lastname: Borcherding
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D042846:CDC2-CDC28 Kinases; D051357:Cyclin-Dependent Kinase 2; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D019073:HT29 Cells / Q000187:drug effects; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D011687:Purines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; C442879:MDL 108522; D010880:Piperidines; D011687:Purines; D017346:Protein Serine-Threonine Kinases; D042846:CDC2-CDC28 Kinases; C495894:CDK2 protein, human; C495893:Cdk2 protein, mouse; D051357:Cyclin-Dependent Kinase 2; D018844:Cyclin-Dependent Kinases; D000225:Adenine