title: Design, synthesis, and biological evaluation of chromone-based p38 MAP kinase inhibitors.
abstract: 3-(4-Fluorophenyl)-2-(4-pyridyl)chromone derivatives were synthesized and evaluated as p38 MAP kinase inhibitors. Introduction of an amino group in the 2-position of the pyridyl moiety gave p38α inhibitors with IC(50) in the low nanomolar range (e.g., IC(50) = 17 nm). The inhibitors showed excellent selectivity profiles when tested on a panel of 62 kinases, as well as efficient inhibition of p38 signaling in human breast cancer cells.
authors: Department of Chemistry, Medicinal Chemistry, University of Gothenburg, SE-41296 Göteborg, Sweden.
authors: Christine
authors: C
authors: Dyrager
authors: Linda Nilsson
authors: LN
authors: Möllers
authors: Linda Karlsson
authors: LK
authors: Kjäll
authors: John Patrick
authors: JP
authors: Alao
authors: Peter
authors: P
authors: Dinér
authors: Fredrik K
authors: FK
authors: Wallner
authors: Per
authors: P
authors: Sunnerhagen
authors: Morten
authors: M
authors: Grøtli
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001943:Breast Neoplasms; D045744:Cell Line, Tumor; D002867:Chromones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D008958:Models, Molecular; D013329:Structure-Activity Relationship; D048051:p38 Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*
chemical_list: D000970:Antineoplastic Agents; D002867:Chromones; D048051:p38 Mitogen-Activated Protein Kinases