2023
DOI: 10.3390/ph16020146
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Metabolism-Guided Optimization of Tryptophanol-Derived Isoindolinone p53 Activators

Abstract: For the first time, the pharmacokinetic (PK) profile of tryptophanol-derived isoindolinones, previously reported as p53 activators, was investigated. From the metabolites’ identification, performed by liquid chromatography coupled to high resolution tandem mass spectrometry (LC-HRMS/MS), followed by their preparation and structural elucidation, it was possible to identify that the indole C2 and C3 are the main target of the cytochrome P450 (CYP)-promoted oxidative metabolism in the tryptophanol-derived isoindo… Show more

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Cited by 4 publications
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