A step-wise synthetic approach is necessary to access γ-conjugates of folate: folate-conjugated prodigiosenes.

Fiche publication


Date publication

mai 2019

Journal

RSC advances

Auteurs

Membres identifiés du Cancéropôle Est :
Dr FIGLIOLA Carlotta


Tous les auteurs :
Figliola C, Marchal E, Groves BR, Thompson A

Résumé

Despite the vast literature that describes reacting folic acid with a pharmacophore, this route is ineffective in providing the correct regioisomer of the resulting conjugate. We herein present a step-wise route to the preparation of nine folate conjugates of the tripyrrolic prodigiosene skeleton. The strict requirement for step-wise construction of the folate core is demonstrated, so as to achieve conjugation at only the desired γ-carboxylic acid and thus maintain the α-carboxylic site for folate receptor (FRα) recognition. Linkages ethylenediamine, polyethylene glycol and glutathione are demonstrated.

Référence

RSC Adv. 2019 05 7;9(25):14078-14092