Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.

Kazutomo Kinoshita,Yoshiyuki Ono,Takashi Emura,Kohsuke Asoh,Noriyuki Furuichi,Toshiya Ito,Hatsuo Kawada,Shota Tanaka,Kenji Morikami,Toshiyuki Tsukaguchi,Hiroshi Sakamoto,Takuo Tsukuda,Nobuhiro Oikawa

Bioorganic & Medicinal Chemistry Letters（2011）

引用 31|浏览21

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摘要

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 21nM and significant antitumor efficacy in ALK fusion-positive blood and solid cancer xenograft models in mice without body weight loss.

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关键词

Anaplastic lymphoma kinase,Kinase inhibitors,Antitumor efficacy

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