Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (1)

…, T Tamura, T Kawamoto, T Tanaka, S Sogabe…

文献索引：Asano, Yasutomi; Kitamura, Shuji; Ohra, Taiichi; Aso, Kazuyoshi; Igata, Hideki; Tamura, Tomoko; Kawamoto, Tomohiro; Tanaka, Toshimasa; Sogabe, Satoshi; Matsumoto, Shin-ichi; Yamaguchi, Masashi; Kimura, Hiroyuki; Itoh, Fumio Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 8 p. 4715 - 4732

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被引用次数: 16

摘要

A novel series of 4-phenylisoquinolones were synthesized and evaluated as c-Jun N- terminal kinase (JNK) inhibitors. Initial modification at the 2-and 3-positions of the isoquinolone ring of hit compound 4, identified from high-throughput screening, led to the lead compound 6b. The optimization was carried out using a JNK1-binding model of 6b and several compounds exhibited potent JNK inhibition. Among them, 11g significantly ...