Structural analysis and biological activities of C25-amino and C25-nitro vitamin D analogs.

Date publication

avril 2023

Journal

Bioorganic chemistry

Auteurs

Membres identifiés du Cancéropôle Est :
Dr ROCHEL-GUIBERTEAU Natacha

Tous les auteurs :
Gómez-Bouzó U, Belorusova AY, Rivadulla ML, Santalla H, Verlinden L, Verstuyf A, Ferronato MJ, Curino AC, Facchinetti MM, Fall Y, Gómez G, Rochel N

Lien Pubmed

https://www.ncbi.nlm.nih.gov/pubmed/37054528

Résumé

Intense synthetic efforts have been directed towards the development of noncalcemic analogs of 1,25-dihydroxyvitamin D. We describe here the structural analysis and biological evaluation of two derivatives of 1,25-dihydroxyvitamin D with modifications limited to the replacement of the 25-hydroxyl group by a 25-amino or 25-nitro groups. Both compounds are agonists of the vitamin D receptor. They mediate biological effects similar to 1,25-dihydroxyvitamin D, the 25-amino derivative being the most potent one while being less calcemic than 1,25-dihydroxyvitamin D. The in vivo properties of the compounds make them of potential therapeutic value.

Référence

Bioorg Chem. 2023 04 6;136:106528