title: Entry into a new class of protein kinase inhibitors by pseudo ring design.
abstract: A pyrimidin-4-yl-urea motif forming a pseudo ring by intramolecular hydrogen bonding has been designed to mimic the pyrido[2,3-d]pyrimidin-7-one core structure of a well-established class of protein kinase inhibitors. Potent inhibition of a number of protein kinases was obtained with the first prototype compound synthesized to probe the design concept.
authors.affiliation: Novartis Institutes for BioMedical Research, WKL-136.P.12, CH-4002 Basel, Switzerland. pascal.furet@novartis.com
authors.forename: Pascal
authors.initials: P
authors.lastname: Furet
authors.forename: Giorgio
authors.initials: G
authors.lastname: Caravatti
authors.forename: Vito
authors.initials: V
authors.lastname: Guagnano
authors.forename: Marc
authors.initials: M
authors.lastname: Lang
authors.forename: Thomas
authors.initials: T
authors.lastname: Meyer
authors.forename: Joseph
authors.initials: J
authors.lastname: Schoepfer
mesh_terms: D000596:Amino Acids / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D008958:Models, Molecular; D008968:Molecular Conformation; D018716:Molecular Mimicry; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011728:Pyridones / Q000737:chemistry* / Q000494:pharmacology*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000596:Amino Acids; C109647:PD 166285; D047428:Protein Kinase Inhibitors; D011728:Pyridones; D011743:Pyrimidines; D014508:Urea