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

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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关键词
anaplastic lymphoma kinase”,inhibitors
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