Synthesis, Molecular Docking and Biological Evaluation of A-Ring-Carborane-Vitamin D Analogues

The active form of vitamin D<sub>3</sub>, 1α,25-dihydroxyvitamin D<sub>3</sub> (1,25D<sub>3</sub>), regulates a number of physiological and pathological processes, including cell proliferation and differentiation. Thousands of analogues of 1,25D<sub>3</sub> 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 <i>ortho</i>-carborane (dicarba-<i>o</i>-<i>closo</i>-1,2-dodecaborane) units. The ligands function as agonists for VDR with similar antiproliferative activities as 1,25D<sub>3</sub>. Whereas mice treated with the analogues <b>4</b> and <b>5</b> exhibited similar hypercalcemic activities as 1,25D<sub>3</sub>, only compound <b>4</b> and 1,25D<sub>3</sub> induced the strong activation of CYP24A1 mRNA expression but not compound <b>5</b>.

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Publication Details

Journal
Molecules
Published
2025-06-18
DOI
https://doi.org/10.3390/molecules30122637
Primary Topic
Boron Compounds in Chemistry
Type
article
Field-Weighted Citation Impact
0.00

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article

Synthesis, Molecular Docking and Biological Evaluation of A-Ring-Carborane-Vitamin D Analogues

Carole Peluso‐Iltis, Maxime Bourguet, Antonio Mouriño, Román Pérez-Fernández et al.
Molecules
Boron Compounds in Chemistry
article

Synthesis, Molecular Docking and Biological Evaluation of A-Ring-Carborane-Vitamin D Analogues

Carole Peluso‐Iltis, Maxime Bourguet, Antonio Mouriño, Román Pérez-Fernández, Natacha Rochel, M.A. Maestro, Samuel Seoane, Sarah Cianférani, R. Moreno Otero, Xoán Fernández-Domínguez
article en

Abstract

The active form of vitamin D<sub>3</sub>, 1α,25-dihydroxyvitamin D<sub>3</sub> (1,25D<sub>3</sub>), regulates a number of physiological and pathological processes, including cell proliferation and differentiation. Thousands of analogues of 1,25D<sub>3</sub> 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 <i>ortho</i>-carborane (dicarba-<i>o</i>-<i>closo</i>-1,2-dodecaborane) units. The ligands function as agonists for VDR with similar antiproliferative activities as 1,25D<sub>3</sub>. Whereas mice treated with the analogues <b>4</b> and <b>5</b> exhibited similar hypercalcemic activities as 1,25D<sub>3</sub>, only compound <b>4</b> and 1,25D<sub>3</sub> induced the strong activation of CYP24A1 mRNA expression but not compound <b>5</b>.

MoleculesVol. 30(12)
Universidade da Coruña (ES), Centre National de la Recherche Scientifique (FR), Inserm (FR), Universidade de Santiago de Compostela (ES), Institut de génétique et de biologie moléculaire et cellulaire (FR), Center for Research in Molecular Medicine and Chronic Diseases (ES), Université de Strasbourg (FR)
Agence Nationale de la Recherche, Université de Strasbourg, Xunta de Galicia
Openalex Percentile: Top 79%
Boron Compounds in Chemistry
DOIOpen Access PDFOpenAlex
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Synthesis, Molecular Docking and Biological Evaluation of A-Ring-Carborane-Vitamin D Analogues — Carole Peluso‐Iltis, Maxime Bourguet, et al. · Molecules (2025) | TGRS Research Map | TGRS