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

Article

Authorship
Gómez-Bouzó, Uxía ; Belorusova, Anna Y. ; Rivadulla, Marcos L. ; Santalla, Hugo ; Verlinden, Lieve ; Verstuyf, Annemieke ; Ferronato, Maria J ; Curino, Alejandro C. ; FACCHINETTI, MARIA MARTA ; Fall, Yagamare ; Gómez, Generosa ; Rochel, Natacha
Date
2023
Publishing House and Editing Place
ACADEMIC PRESS INC ELSEVIER SCIENCE
Magazine
BIOORGANIC CHEMISTRY, vol. 136 ACADEMIC PRESS INC ELSEVIER SCIENCE
Summary Information provided by the agent in SIGEVA
Intense synthetic efforts have been directed towards the development of noncalcemic analogs of 1,25-dihydroxyvitamin D3. We describe here the structural analysis and biological evaluation of two derivatives of 1,25-dihydroxyvitamin D3 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 D3, the 25-amino derivative being the m... Intense synthetic efforts have been directed towards the development of noncalcemic analogs of 1,25-dihydroxyvitamin D3. We describe here the structural analysis and biological evaluation of two derivatives of 1,25-dihydroxyvitamin D3 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 D3, the 25-amino derivative being the most potent one while being less calcemic than 1,25-dihydroxyvitamin D3. The in vivo properties of the compounds make them of potential therapeutic value.
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Key Words
VDRANALOGSVITAMIN DBIOLOGICAL ACTIVITY