Discovery of Novel α-Carboline Inhibitors of the Anaplastic Lymphoma Kinase.

Luca Mologni,Sébastien Tardy,Alfonso Zambon,Alexandre Orsato,William H Bisson,Monica Ceccon,Michela Viltadi, Joseph D'Attoma,Sara Pannilunghi,Vito Vece,Jerome Bertho,Peter Goekjian,Leonardo Scapozza,Carlo Gambacorti-Passerini

ACS Omega（2022）

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摘要

The anaplastic lymphoma kinase (ALK) is abnormally expressed and hyperactivated in a number of tumors and represents an ideal therapeutic target. Despite excellent clinical responses to ALK inhibition, drug resistance still represents an issue and novel compounds that overcome drug-resistant mutants are needed. We designed, synthesized, and evaluated a large series of azacarbazole inhibitors. Several lead compounds endowed with submicromolar potency were identified. Compound 149in vitro149

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