title: Novel triazole based inhibitors of Ras farnesyl transferase.
abstract: A novel series of potent inhibitors of Ras farnesyl transferase possessing a 1,2,4-triazole pharmacophore is described. These inhibitors were discovered from a parallel synthesis effort and were subsequently optimized to in vitro IC(50) value of less than 1nM.
authors.affiliation: Department of Medicinal Chemistry, Janssen Research Foundation, Johnson & Johnson Pharmaceutical Research & Development, Welsh and McKean Roads, Spring House, PA 19477, USA. asaha@predixpharm.com
authors.forename: Ashis K
authors.initials: AK
authors.lastname: Saha
authors.forename: Li
authors.initials: L
authors.lastname: Liu
authors.forename: Richard
authors.initials: R
authors.lastname: Simoneaux
authors.forename: Bart
authors.initials: B
authors.lastname: DeCorte
authors.forename: Christophe
authors.initials: C
authors.lastname: Meyer
authors.forename: Stacy
authors.initials: S
authors.lastname: Skrzat
authors.forename: Henry J
authors.initials: HJ
authors.lastname: Breslin
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Kukla
authors.forename: Dave W
authors.initials: DW
authors.lastname: End
mesh_terms: D000595:Amino Acid Sequence; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D051231:Farnesyltranstransferase / Q000037:antagonists & inhibitors* / Q000235:genetics; D011905:Genes, ras; D008958:Models, Molecular; D008968:Molecular Conformation; D009842:Oligopeptides / Q000737:chemistry; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D009842:Oligopeptides; D014230:Triazoles; D051231:Farnesyltranstransferase