A环碳硼烷 - 维生素D类似物的合成、分子对接及生物学评价
Synthesis, Molecular Docking and Biological Evaluation of A-Ring-Carborane-Vitamin D Analogues.
作者信息
Otero Rocío, Seoane Samuel, Fernández-Domínguez Xoán, Bourguet Maxime, Cianférani Sarah, Peluso-Iltis Carole, Maestro Miguel A, Pérez-Fernández Román, Rochel Natacha, Mouriño Antonio
机构信息
Ignacio Ribas Research Laboratory, Department of Organic Chemistry, University of Santiago de Compostela, 15782 Santiago de Compostela, Spain.
Department of Physiology-Center for Research in Molecular Medicine and Chronic Diseases (CIMUS), University of Santiago de Compostela, 15707 Santiago de Compostela, Spain.
出版信息
Molecules. 2025 Jun 18;30(12):2637. doi: 10.3390/molecules30122637.
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 .
维生素D的活性形式，1α,25-二羟基维生素D（1,25D），调节许多生理和病理过程，包括细胞增殖和分化。为了实现医学用途的选择性作用，人们已经开发了数千种1,25D类似物。在此，我们描述了两种带有 -碳硼烷（二碳 - - - 1,2 - 十二硼烷）单元的新型非传统A环修饰维生素D类似物的合成。这些配体作为维生素D受体（VDR）的激动剂，具有与1,25D相似的抗增殖活性。用类似物 和 处理的小鼠表现出与1,25D相似的高钙血症活性，只有化合物 和1,25D诱导CYP24A1 mRNA表达的强烈激活，而化合物 则不然。
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