Design and synthesis of novel allosteric MEK inhibitor CH4987655 as an orally available anticancer agent

…, S Tsujii, K Hattori, T Miura, Y Yoshimura, S Aida…

文献索引：Isshiki, Yoshiaki; Kohchi, Yasunori; Iikura, Hitoshi; Matsubara, Yasuaki; Asoh, Kohsuke; Murata, Takeshi; Kohchi, Masami; Mizuguchi, Eisaku; Tsujii, Shinji; Hattori, Kazuo; Miura, Takaaki; Yoshimura, Yasushi; Aida, Satoshi; Miwa, Masanori; Saitoh, Ryoichi; Murao, Naoaki; Okabe, Hisafumi; Belunis, Charles; Janson, Cheryl; Lukacs, Christine; Schueck, Verena; Shimma, Nobuo Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 6 p. 1795 - 1801

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被引用次数: 48

摘要

The MAP kinase pathway is one of the most important pathways involved in cell proliferation and differentiation, and its components are promising targets for antitumor drugs. Design and synthesis of a novel MEK inhibitor, based on the 3D-structural information of the target enzyme, and then multidimensional optimization including metabolic stability, physicochemical properties and safety profiles were effectively performed and led to the ...