title: Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.
abstract: Benzimidazole reverse amides were designed and synthesized as Pan RAF kinase inhibitors. Investigation of the structure-activity relationship of the compounds revealed that they were potent in vitro and exhibited desirable in vivo properties.
authors.affiliation: Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research , 4560 Horton Street, Emeryville, California 94608, United States.
authors.forename: Sharadha
authors.initials: S
authors.lastname: Subramanian
authors.affiliation: Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research , 4560 Horton Street, Emeryville, California 94608, United States.
authors.forename: Abran
authors.initials: A
authors.lastname: Costales
authors.affiliation: Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research , 4560 Horton Street, Emeryville, California 94608, United States.
authors.forename: Teresa E
authors.initials: TE
authors.lastname: Williams
authors.affiliation: Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research , 4560 Horton Street, Emeryville, California 94608, United States.
authors.forename: Barry
authors.initials: B
authors.lastname: Levine
authors.affiliation: Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research , 4560 Horton Street, Emeryville, California 94608, United States.
authors.forename: Christopher M
authors.initials: CM
authors.lastname: McBride
authors.affiliation: Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research , 4560 Horton Street, Emeryville, California 94608, United States.
authors.forename: Daniel
authors.initials: D
authors.lastname: Poon
authors.affiliation: Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research , 4560 Horton Street, Emeryville, California 94608, United States.
authors.forename: Payman
authors.initials: P
authors.lastname: Amiri
authors.affiliation: Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research , 4560 Horton Street, Emeryville, California 94608, United States.
authors.forename: Paul A
authors.initials: PA
authors.lastname: Renhowe
authors.affiliation: Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research , 4560 Horton Street, Emeryville, California 94608, United States.
authors.forename: Cynthia M
authors.initials: CM
authors.lastname: Shafer
authors.affiliation: Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research , 4560 Horton Street, Emeryville, California 94608, United States.
authors.forename: Darrin
authors.initials: D
authors.lastname: Stuart
authors.affiliation: Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research , 4560 Horton Street, Emeryville, California 94608, United States.
authors.forename: Joelle
authors.initials: J
authors.lastname: Verhagen
authors.affiliation: Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research , 4560 Horton Street, Emeryville, California 94608, United States.
authors.forename: Savithri
authors.initials: S
authors.lastname: Ramurthy
keywords: CSF1R; MAP; RTKs; STKs; TKs; VEGF; colony stimulating factor-1 receptor; ras-mitogen activated protein kinase; receptor tyrosine kinases; serine threonine kinases; tyrosine kinases; vascular endothelial growth factor receptor