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Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors |
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| Authors: | Kinoshita Kazutomo Ono Yoshiyuki Emura Takashi Asoh Kohsuke Furuichi Noriyuki Ito Toshiya Kawada Hatsuo Tanaka Shota Morikami Kenji Tsukaguchi Toshiyuki Sakamoto Hiroshi Tsukuda Takuo Oikawa Nobuhiro |
| Institution: | a Kamakura Research Laboratories, Chugai Pharmaceutical Co. Ltd., 200 Kajiwara, Kamakura, Kanagawa 247-8530, Japan b Fuji-Gotemba Research Laboratories, Chugai Pharmaceutical Co. Ltd., 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan |
| Abstract: | Anaplastic lymphoma kinase (ALK) receptor tyrosine kinase is considered a promising therapeutic target for human cancers. We identified novel tetracyclic derivatives as potent ALK inhibitors. Among them, compound 27 showed strong cytotoxicity against KARPAS-299 with an IC50 value of 21 nM and significant antitumor efficacy in ALK fusion-positive blood and solid cancer xenograft models in mice without body weight loss. |
| Keywords: | Anaplastic lymphoma kinase Kinase inhibitors Antitumor efficacy |
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