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首页> 外文期刊>Organometallics >Synthesis, crystal structure analysis, and pharmacological characterization of disila-bexarotene, a disila-analogue of the RXR-selective retinoid agonist bexarotene
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Synthesis, crystal structure analysis, and pharmacological characterization of disila-bexarotene, a disila-analogue of the RXR-selective retinoid agonist bexarotene

机译：RXR-选择性类维生素A激动剂贝沙罗汀的二硅氮类似物二硅-贝沙罗丁的合成，晶体结构分析和药理学表征

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摘要

Twofold sila-substitution (C/Si exchange) in the saturated ring of the tetrahydronaphthalene skeleton of the RXR-selective retinoid agonist bexarotene (1a) leads to disilabexarotene (1b). Compound 1b was synthesized in a multistep synthesis, starting from 1,2-bis(chlorodimethylsilyl)ethane. The identity of 1b was established by elemental analyses and multinuclear NMR studies, and the C/Si analogues 1a and 1b (and an intermediate in the synthesis of 1b) were structurally characterized by single-crystal X-ray diffraction. Furthermore, 1a and 1b were studied for their interaction with retinoid X receptors. Although the twofold sila-substitution of la resulted in significant differences in the molecular structures of 1a and 1b, disila-bexarotene (1b) was shown to be a highly potent RXR agonist.
机译：RXR选择性类维生素A激动剂贝沙罗汀（1a）的四氢萘骨架的饱和环中的两倍sila取代（C / Si交换）会导致二硅拉贝沙罗汀（1b）。从1，2-双（氯二甲基甲硅烷基）乙烷开始，以多步合成法合成化合物1b。通过元素分析和多核NMR研究确定1b的身份，并通过单晶X射线衍射对C / Si类似物1a和1b（以及1b合成中的中间体）进行结构表征。此外，研究了1a和1b与类维生素A X受体的相互作用。虽然1a的双重sila取代导致1a和1b的分子结构发生显着差异，但二硅-贝沙罗汀（1b）被证明是高效RXR激动剂。

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