Scaffold hopping approach to a new series of smoothened antagonists

LuW.; GengD.; SunZ.; YangZ.; MaH.; ZhengJ.; ZhangX.

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Scaffold hopping approach to a new series of smoothened antagonists

机译：脚手架跳跃方法是一系列新的平滑拮抗剂

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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期间的关键调节因子，而在成人中，其功能有限，如干细胞维护和组织修复。成人中HH信号传导的异常活性与众不同。因此，对HH信号传导的抑制代表了新的抗癌疗法的有希望的方法。平滑的（Smo）受体介导HH信号传导。在这里，我们报告了通过脚手架跳跃策略获得的一系列新的SMO拮抗剂。来自这种新支架的化合物证明了对HH途径信号的体面抑制。新脚手架可以作为进一步优化的起点。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2014年第10期|共5页
作者
LuW.; GengD.; SunZ.; YangZ.; MaH.; ZhengJ.; ZhangX.;
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作者单位

Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases College of;

Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases College of;

BeiGene (Beijing) Co. Ltd Zhongguancun Life Science Park No. 30 Science Park Road Beijing 102206;

Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases College of;

Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases College of;

Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases College of;

Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases College of;

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正文语种 eng
中图分类药学;
关键词
Antagonist; Cancer therapy; GPCR; Hedgehog pathway; Scaffold hopping; Smoothened;

机译：拮抗剂;癌症治疗;GPCR;刺猬途径;脚手架跳跃;平滑;

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专利

1. Scaffold hopping approach to a new series of smoothened antagonists [J] . LuW., GengD., SunZ., Bioorganic and Medicinal Chemistry Letters . 2014,第10期

机译：脚手架跳跃方法是一系列新的平滑拮抗剂
2. Design and synthesis of a novel series of histamine H-3 receptor antagonists through a scaffold hopping strategy [J] . Gao Zhongli, Hurst William J., Hall Daniel, Bioorganic and medicinal chemistry . 2015,第3期

机译：通过支架跳跃策略设计和合成一系列新的组胺H-3受体拮抗剂
3. Scaffold-hopping with zwitterionic CCR3 antagonists: Identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092 [J] . BahlA., BartonP., BowersK., Bioorganic and Medicinal Chemistry Letters . 2012,第21期

机译：铲斗跳跃与两倍离子CCR3拮抗剂：识别和优化系列，具有良好的效力和药代动力学，导致AZ12436092的发现
4. Single Parameter Exponential Time Series Smoothening to Dampen Wind Power Irregularities in Grid-Integrated Doubly Fed Induction Generator [C] . Souvik Das, Sambasivaiah Puchalapalli, Bhim Singh, IEEE International Conference on Power Electronics, Smart Grid and Renewable Energy . 2020

机译：并网双馈感应发电机中单参数指数时间序列平滑化以抑制风电不规则性
5. Application of organocatalysis to the synthesis of pharmaceutically relevant scaffolds: Chiral aziridines and beta-fluoroamines; total synthesis of stemaphylline; and discovery of selective PAR4 antagonists. [D] . Schulte, Michael L. 2013

机译：有机催化在药物相关支架合成中的应用：手性氮丙啶和β-氟胺；茶碱的全合成；和发现选择性PAR4拮抗剂。
6. Pharmacological evaluation of a series of smoothened antagonists in signaling pathways and after topical application in a depilated mouse model [O] . Emilie Lauressergues, †, Peter Heusler, 2016

机译：在脱毛的小鼠模型中一系列平滑化拮抗剂在信号传导途径中和局部应用后的药理学评价
7. Scaffold Hopping with Molecular Field Points: Identification of a Cholecystokinin-2 (CCK2) Receptor Pharmacophore and Its Use in the Design of a Prototypical Series of Pyrrole- and Imidazole-Based CCK2 Antagonists [O] . -1

机译：与分子场点的脚手架跳跃：鉴别胆囊蛋白-2（CCK2）受体药物团及其在设计吡咯和咪唑基CCK2拮抗剂的设计中的设计

Scaffold hopping approach to a new series of smoothened antagonists

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