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ID: ALA1777813

Journal: Bioorg Med Chem Lett

Title: Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.

Authors: Kinoshita K, Ono Y, Emura T, Asoh K, Furuichi N, Ito T, Kawada H, Tanaka S, Morikami K, Tsukaguchi T, Sakamoto H, Tsukuda T, Oikawa N.

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 IC(50) value of 21 nM and significant antitumor efficacy in ALK fusion-positive blood and solid cancer xenograft models in mice without body weight loss.

CiteXplore: 21561771

DOI: 10.1016/j.bmcl.2011.04.020