FIELD: chemistry.
SUBSTANCE: invention relates to a method of producing a bifunctional conjugate SNIPER based on a cabozantinib inhibitor, involving synthesis of a cabozantinib derivative, containing a linker with a hydroxyl group, which is N-(4-fluorophenyl)-N-(((7-(3-(3-hydroxypropoxy)propoxy)propoxy)-6-methoxyquinolin-4-yl)oxy)phenyl)cyclopropane-1,1-dicarboxamide.
EFFECT: method enables to obtain a novel bifunctional conjugate based on a cabozantinib inhibitor and a ligand for IAP protein based on (S)-N-((S)-1-cyclohexyl-2-oxo-2-((S)-2-(4-phenylthiazol-2-yl)pyrrolidin-1-yl)ethyl)-2-(methylamino))-propanamide, linked to each other by a polypropylene glycol linker, providing the binding between the target pathogenic protein c-Met and the IAP protein as E3-ligase with subsequent polyubiquitination, transport into the proteasome and splitting of the target protein c-Met.
1 cl, 5 dwg, 1 ex
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Authors
Dates
2025-04-11—Published
2023-11-02—Filed