title: Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines.
abstract: The identification of 2-pyridinylguanidines (e.g., 27 and 28) as selective inhibitors of urokinase-type plasminogen activator (uPA) is described. The X-ray crystal structure of 27 has been determined, and modelling has been used to predict binding in the enzyme active site.
authors.affiliation: Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich, Kent CT13 9NJ, UK. christopher_barber@sandwich.pfizer.com
authors.forename: Christopher G
authors.initials: CG
authors.lastname: Barber
authors.forename: Roger P
authors.initials: RP
authors.lastname: Dickinson
authors.forename: Valerie A
authors.initials: VA
authors.lastname: Horne
mesh_terms: D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006146:Guanidines / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D011725:Pyridines / Q000737:chemistry*; D014568:Urokinase-Type Plasminogen Activator / Q000037:antagonists & inhibitors*; D014961:X-Ray Diffraction
chemical_list: D004791:Enzyme Inhibitors; D006146:Guanidines; D011725:Pyridines; D014568:Urokinase-Type Plasminogen Activator; C023666:pyridine