A novel bioresponsive self-immolative spacer based on aza-quinone methide reactivity for the controlled release of thiols, phenols, amines, sulfonamides or amides
Elena Ermini, Annalaura Brai, Elena Cini, Federica Finetti, Giuseppe Giannini, Daniele Padula, Lucrezia Paradisi, Federica Poggialini, Lorenza Trabalzini, Paola Tolu, Maurizio Taddei
Abstract
-aminobenzyl derivatives. The NPYM scaffold was validated by late-stage functionalisation of approved drugs such as celecoxib, colchicine, vorinostat or ciprofloxacin. A hypoxia-activated NPYM-based prodrug (HAP) derived from HDAC inhibitor ST7612AA1 was also produced, which was active in cancer cells under hypoxic conditions.
Topics & Concepts
ChemistryQuinone methidePyrroleCombinatorial chemistryReactivity (psychology)PhenolsQuinoneCatalysisOrganic chemistryPathologyAlternative medicineMedicineChemical Synthesis and AnalysisClick Chemistry and ApplicationsChemical Synthesis and Reactions