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

Autor: Gómez-Bouzó U; Departamento de Química Orgánica and Instituto de Investigación Sanitaria Galicia Sur (IISGS), Campus Lagoas Marcosende, Universidad de Vigo, 36310 Vigo, Spain., Belorusova AY; Institut de Génétique et de Biologie Moléculaire et Cellulaire (IGBMC), Institut National de La Santé et de La Recherche Médicale (INSERM), U1258, Centre National de Recherche Scientifique (CNRS), UMR7104, Université de Strasbourg, Strasbourg, Illkirch 67400, France., Rivadulla ML; Departamento de Química Orgánica and Instituto de Investigación Sanitaria Galicia Sur (IISGS), Campus Lagoas Marcosende, Universidad de Vigo, 36310 Vigo, Spain., Santalla H; Departamento de Química Orgánica and Instituto de Investigación Sanitaria Galicia Sur (IISGS), Campus Lagoas Marcosende, Universidad de Vigo, 36310 Vigo, Spain., Verlinden L; Clinical and Experimental Endocrinology, Department of Chronic Diseases and Metabolism, KU Leuven, 3000 Leuven, Belgium., Verstuyf A; Clinical and Experimental Endocrinology, Department of Chronic Diseases and Metabolism, KU Leuven, 3000 Leuven, Belgium., Ferronato MJ; Laboratorio de Biología del Cáncer, Instituto de Investigaciones Bioquímicas Bahía Blanca (INIBIBB-CONICET), Centro Científico Tecnológico Bahía Blanca, Bahía Blanca, Argentina., Curino AC; Laboratorio de Biología del Cáncer, Instituto de Investigaciones Bioquímicas Bahía Blanca (INIBIBB-CONICET), Centro Científico Tecnológico Bahía Blanca, Bahía Blanca, Argentina., Facchinetti MM; Laboratorio de Biología del Cáncer, Instituto de Investigaciones Bioquímicas Bahía Blanca (INIBIBB-CONICET), Centro Científico Tecnológico Bahía Blanca, Bahía Blanca, Argentina., Fall Y; Departamento de Química Orgánica and Instituto de Investigación Sanitaria Galicia Sur (IISGS), Campus Lagoas Marcosende, Universidad de Vigo, 36310 Vigo, Spain., Gómez G; Departamento de Química Orgánica and Instituto de Investigación Sanitaria Galicia Sur (IISGS), Campus Lagoas Marcosende, Universidad de Vigo, 36310 Vigo, Spain. Electronic address: ggomez@uvigo.es., Rochel N; Institut de Génétique et de Biologie Moléculaire et Cellulaire (IGBMC), Institut National de La Santé et de La Recherche Médicale (INSERM), U1258, Centre National de Recherche Scientifique (CNRS), UMR7104, Université de Strasbourg, Strasbourg, Illkirch 67400, France. Electronic address: rochel@igbmc.fr.
Jazyk: angličtina
Zdroj: Bioorganic chemistry [Bioorg Chem] 2023 Jul; Vol. 136, pp. 106528. Date of Electronic Publication: 2023 Apr 06.
DOI: 10.1016/j.bioorg.2023.106528
Abstrakt: Intense synthetic efforts have been directed towards the development of noncalcemic analogs of 1,25-dihydroxyvitamin D 3 . We describe here the structural analysis and biological evaluation of two derivatives of 1,25-dihydroxyvitamin D 3 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 3 , the 25-amino derivative being the most potent one while being less calcemic than 1,25-dihydroxyvitamin D 3 . The in vivo properties of the compounds make them of potential therapeutic value.
Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2023 Elsevier Inc. All rights reserved.)
Databáze: MEDLINE
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