title: Synthesis of novel 1,4-benzoxazin-3-one derivatives as inhibitors against tyrosine kinases.
abstract: We designed and synthesized a novel 1,4-benzoxazin-3-one derivative 4 which would have inhibitory activities against tyrosine kinases. They could be synthesized easily from various carboxylic acids 10 and commercially available amines using TFP resin without purification. In this article, we will report the design and synthesis of a novel 1,4-benzoxazin-3-one chemical library 4 and the inhibitory activities against KDR and ABL which are closely related to chronic diseases such as cancer.
authors.affiliation: Research and Development Center, Santen Pharmaceutical Co. Ltd, 8916-16 Takayama-cho, Ikoma-shi, Nara 630-0101, Japan. hondat@ms.naist.jp
authors.forename: Takahiro
authors.initials: T
authors.lastname: Honda
authors.forename: Takahiro
authors.initials: T
authors.lastname: Terao
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Aono
authors.forename: Masakazu
authors.initials: M
authors.lastname: Ban
mesh_terms: D000588:Amines; D048588:Benzoxazines / Q000138:chemical synthesis* / Q000494:pharmacology; D002264:Carboxylic Acids; D015195:Drug Design; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D016315:Proto-Oncogene Proteins c-abl / Q000037:antagonists & inhibitors; D054852:Small Molecule Libraries / Q000138:chemical synthesis; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors
chemical_list: D000588:Amines; D048588:Benzoxazines; D002264:Carboxylic Acids; D054852:Small Molecule Libraries; D011505:Protein-Tyrosine Kinases; D040301:Vascular Endothelial Growth Factor Receptor-2; D016315:Proto-Oncogene Proteins c-abl