Fiche publication
Date publication
juin 2025
Journal
Molecules (Basel, Switzerland)
Auteurs
Membres identifiés du Cancéropôle Est :
Dr CIANFERANI Sarah
,
Dr ROCHEL-GUIBERTEAU Natacha
Tous les auteurs :
Otero R, Seoane S, Fernández-Domínguez X, Bourguet M, Cianférani S, Peluso-Iltis C, Maestro MA, Pérez-Fernández R, Rochel N, Mouriño A
Lien Pubmed
Résumé
The active form of vitamin D, 1α,25-dihydroxyvitamin D (1,25D), regulates a number of physiological and pathological processes, including cell proliferation and differentiation. Thousands of analogues of 1,25D have been developed with the aim of selective effects for medical use. Here we describe the synthesis of two new unconventional vitamin D analogues bearing A-ring modifications with -carborane (dicarba---1,2-dodecaborane) units. The ligands function as agonists for VDR with similar antiproliferative activities as 1,25D. Whereas mice treated with the analogues and exhibited similar hypercalcemic activities as 1,25D, only compound and 1,25D induced the strong activation of CYP24A1 mRNA expression but not compound .
Mots clés
A-ring-carboranes, biological activity, docking, synthesis, vitamin D3 analogues, vitamin D3 receptor
Référence
Molecules. 2025 06 18;30(12):
