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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Scaffold hopping approach to a new series of smoothened antagonists
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Scaffold hopping approach to a new series of smoothened antagonists

机译：新的平滑拮抗剂系列的支架跳跃法

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The hedgehog (Hh) signaling pathway is a key regulator during embryonic development, while in adults, it has limited functions such as stem cell maintenance and tissue repair. The aberrant activity of the Hh signaling in adults has been linked to numerous human cancers. Inhibition of Hh signaling therefore represents a promising approach toward novel anticancer therapies. The Smoothened (Smo) receptor mediates Hh signaling. Here we report a new series of Smo antagonists which were obtained by a scaffold hopping strategy. Compounds from this new scaffold demonstrated decent inhibition of Hh pathway signaling. The new scaffold can serve as a starting point for further optimization.
机译：刺猬（Hh）信号通路是胚胎发育过程中的关键调控因子，而在成年人中，其功能有限，例如干细胞维持和组织修复。 Hh信号在成年人中的异常活动已与许多人类癌症有关。因此，抑制Hh信号代表了一种针对新型抗癌疗法的有前途的方法。平滑（Smo）受体介导Hh信号传导。在这里，我们报告了一系列新的Smo拮抗剂，它们是通过支架跳跃策略获得的。来自这种新支架的化合物表现出对Hh途径信号传导的良好抑制。新的脚手架可以作为进一步优化的起点。

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