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首页> 外文期刊>Chemistry: A European journal >An Expeditious Route to 1a,25-Dihydroxyvitamin D_3 and Its Analogues by an Aqueous Tandem Palladium-Catalyzed A-Ring Closure and Suzuki Coupling to the C/D Unit
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An Expeditious Route to 1a,25-Dihydroxyvitamin D_3 and Its Analogues by an Aqueous Tandem Palladium-Catalyzed A-Ring Closure and Suzuki Coupling to the C/D Unit

机译：串联钯水催化的A环封闭和Suzuki偶联到C / D单元的1a，25-二羟基维生素D_3及其类似物的快速合成

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摘要

1a,25-Dihydroxyvitamin D3 (1), the hormonally active metabolite of the seco-steroid vitamin D3, interacts with the vitamin D nuclear receptor (VDR)[1] to initiate a cascade of events that ultimately controls mineral homeostasis and a multitude of cellular processes including differentiation, antiproliferation, growth, apoptosis, angiogenesis, and immunomodulation.[ 2] Unfortunately, the therapeutic applications of 1 in pharmacological doses to correct dysfunction of one or more of these processes are severely limited by its potent calcemic effects.[3] Efforts to develop analogues with selectively reduced calcemic effects for treatment of, for example, cancer and skin diseases or with selective activity on bone formation have led to more than 3000 synthetic analogues being tested, although only a few have reached the pharmaceutical market or advanced clinical trials.
机译：1a，25-二羟基维生素D3（1），是甾类固醇维生素D3的激素活性代谢产物，与维生素D核受体（VDR）相互作用[1]，引发一系列事件，最终控制了矿物质的体内稳态和多种细胞过程，包括分化，抗增殖，生长，凋亡，血管生成和免疫调节。[2]不幸的是，1的药理学剂量在纠正这些过程中一个或多个功能障碍时的治疗应用受到其有效的钙化作用的严重限制。[3] ]开发具有选择性降低钙减少作用的类似物以治疗例如癌症和皮肤病或对骨形成具有选择性活性的努力已导致测试了3000多种合成类似物，尽管只有少数几个进入药物市场或进入临床审判。

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