title: Design and synthesis of 5,6-fused heterocyclic amides as Raf kinase inhibitors.
abstract: Two scaffolds based on 5,6-fused heterocyclic backbones were designed and synthesized as Raf kinase inhibitors. The scaffolds were assessed for in vitro pan-Raf inhibition, activity in cell proliferation and target modulation assays, and pharmacokinetic parameters.
authors.affiliation: Global Discovery Chemistry/Oncology and Exploratory Chemistry, Novartis Institutes for Biomedical Research, 4560 Horton Street, Emeryville, CA 94608, USA. savithri.ramurthy@novartis.com
authors.forename: Savithri
authors.initials: S
authors.lastname: Ramurthy
authors.forename: Mina
authors.initials: M
authors.lastname: Aikawa
authors.forename: Payman
authors.initials: P
authors.lastname: Amiri
authors.forename: Abran
authors.initials: A
authors.lastname: Costales
authors.forename: Ahmad
authors.initials: A
authors.lastname: Hashash
authors.forename: Johanna M
authors.initials: JM
authors.lastname: Jansen
authors.forename: Song
authors.initials: S
authors.lastname: Lin
authors.forename: Sylvia
authors.initials: S
authors.lastname: Ma
authors.forename: Paul A
authors.initials: PA
authors.lastname: Renhowe
authors.forename: Cynthia M
authors.initials: CM
authors.lastname: Shafer
authors.forename: Sharadha
authors.initials: S
authors.lastname: Subramanian
authors.forename: Leonard
authors.initials: L
authors.lastname: Sung
authors.forename: Joelle
authors.initials: J
authors.lastname: Verhagen
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001665:Binding Sites; D049109:Cell Proliferation; D015195:Drug Design; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D048490:raf Kinases / Q000037:antagonists & inhibitors*
chemical_list: D000577:Amides; D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D048490:raf Kinases