1α,25-Dihydroxyvitamin D3-3β-bromoacetate, a potential cancer therapeutic agent: Synthesis and molecular mechanism of action

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:21

Article

Ray, Rahul¹  Lambert, James R.² 

[1] Boston Univ, Sch Med, Dept Med, Boston, MA 02118 USA

[2] Univ Colorado, Dept Pathol, Aurora, CO 80045 USA

关键词: 1 alpha,25-Dihydroxyvitamin D-3 (1,25(OH)(2)D-3);    1 alpha,25-Dihydroxyvitamin D-3-3 beta-bromoacetate (1,25(OH)(2)D-3-3-BE);    Vitamin D receptor (VDR);    Vitamin D receptor-ligand binding domain (VDR-LBD);    Synthesis of 1,25(OH)(2)D-3-3-BE;    Anti-cancer agent;    Mechanism of action of 1,25(OH)(2)D-3-3-BE;    1 alpha,25-Dihydroxyvitamin D-3-24-hydroxylase;    (CYP24);   

DOI  :  10.1016/j.bmcl.2011.02.025

来源: Elsevier

【 摘 要 】

Synthesis of 1 alpha,25-dihydroxyvitamin D-3-3 beta-bromoacetate (1,25(OH)(2)D-3-3-BE), a potential anti-cancer agent is presented. We also report that mechanism of action of 1,25(OH)(2)D-3-3-BE may involve reduction of its catabolism, as evidenced by the reduced and delayed expression of 1 alpha,25-dihydroxyvitamin D-3-24-hydroxylase (CYP24) gene in cellular assays. (C) 2011 Elsevier Ltd. All rights reserved.

【 授权许可】

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