Synthesis, SAR studies, and pharmacological evaluation of 3-anilino-4-(3-indolyl) maleimides with conformationally restricted structure as orally bioavailable PKCβ- …

…, M Takahashi, T Sasase, N Ueda, M Matsushita…

文献索引：Tanaka, Masahiro; Sagawa, Shoichi; Hoshi, Jun-ichi; Shimoma, Fumito; Yasue, Katsutaka; Ubukata, Minoru; Ikemoto, Tomoyuki; Hase, Yasunori; Takahashi, Mitsuru; Sasase, Tomohiko; Ueda, Nobuhisa; Matsushita, Mutsuyoshi; Inaba, Takashi Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 17 p. 5781 - 5794

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被引用次数: 35

摘要

Conformationally restricted 3-anilino-4-(3-indolyl) maleimide derivatives were designed and synthesized aiming at discovery of novel protein kinase Cβ (PKCβ)-selective inhibitors possessing oral bioavailability. Among them, compounds having a fused five-membered ring at the indole 1, 2-position inhibited PKCβ2 with IC50 of nM-order and showed good oral bioavailability. One of the most potent compounds was found to be PKCβ-selective over ...