Synthesis of novel 1,4-benzoxazin-3-one derivatives as inhibitors against tyrosine kinases |
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| Authors: | Takahiro Honda Takahiro Terao Hiroyuki Aono Masakazu Ban |
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| Institution: | 1. Research and Development Center, Santen Pharmaceutical Co. Ltd, 8916-16 Takayama-cho, Ikoma-shi, Nara 630-0101, Japan;2. Graduate School of Materials Sciences, Nara Institute of Science and Technology, 8916-5 Takayama-cho, Ikoma-shi, Nara 630-0192, Japan |
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| 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. |
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