Synthesis of novel 1,4-benzoxazin-3-one derivatives as inhibitors against tyrosine kinases.
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.
Honda
Takahiro
T
Research and Development Center, Santen Pharmaceutical Co. Ltd, 8916-16 Takayama-cho, Ikoma-shi, Nara 630-0101, Japan. hondat@ms.naist.jp
Terao
Takahiro
T
Aono
Hiroyuki
H
Ban
Masakazu
M
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
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