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黑 (Hh) 信号通路抑制剂环胺的不对称合成

Hao Shao¹, Wenheng Liu², Muhan Liu³

¹Shanghai Key Laboratory of Green Chemistry and Chemical Processes, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China.

Journal of the American Chemical Society

|November 10, 2023

概括

研究人员用一种新的两级中继策略合成了虫 (Hh) 信号通路的类固醇胺. 通过向Hh信号来开发新的癌症疗法.

科学领域:

有机化学
医学化学
分子生物学

背景情况:

环胺是一种类固醇类化合物.
它通过向Smo受体来抑制刺 (Hh) 信号通路.
抑制子通路是一种治疗癌症的策略.

研究的目的:

报告环胺的不对称合成.
开发一个双阶段的循环胺合成中继策略.

主要方法:

第一个阶段是通过融合方法对维拉特的总合成.
一个关键的光诱导激发状态纳扎罗夫反应被用来构建C-nor-D-homo-steroid骨架.
通过化学选择性氧化还原操作将维拉特胺转化为环胺.

主要成果:

成功实现了环胺的不对称合成.
建立了合成的两阶段中继策略.

结论:

开发的合成途径提供了循环胺.
这种合成是开发针对Hh途径的新型癌症治疗方法的关键一步.

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