A novel bioresponsive self-immolative spacer based on aza-quinone methide reactivity for the controlled release of thiols, phenols, amines, sulfonamides or amides

Author:

Ermini Elena1ORCID,Brai Annalaura1ORCID,Cini Elena1ORCID,Finetti Federica1,Giannini Giuseppe2,Padula Daniele1ORCID,Paradisi Lucrezia1,Poggialini Federica1,Trabalzini Lorenza1,Tolu Paola1,Taddei Maurizio1ORCID

Affiliation:

1. Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via A. Moro 2, 53100 Siena, Italy

2. Translational Medicine & Clinical Pharmacology Corporate R&D – Alfasigma SpA, Via Pontina, km 30400, 00071 Pomezia (Roma), Italy

Abstract

The power of pyrrole: a 1,6-self-immolative spacer designed on the pyrrole structure enables direct late-stage functionalisation of drugs and their traceless release under enzymatic or reductive micellar catalysis in water.

Publisher

Royal Society of Chemistry (RSC)

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