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Synthesis and Smo Activity of Some Novel Benzamide Derivatives

Two series of benzamides compounds bearing piperidine groups were synthesized and the Gli-luc luciferase activity was screened by Gys-luc luciferase gene detection method. Compound 5q showed promising inhibition of hedgehog (Hh) signaling pathway. To further verify whether the Hh inhibitory activiti...

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Autores principales: Ding, Huaiwei, Chen, Kai, Song, Bingke, Deng, Chenglong, Li, Wei, Niu, Li, Bai, Mengxuan, Song, Hongrui, Zhang, Lijuan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017536/
https://www.ncbi.nlm.nih.gov/pubmed/29301237
http://dx.doi.org/10.3390/molecules23010085
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author Ding, Huaiwei
Chen, Kai
Song, Bingke
Deng, Chenglong
Li, Wei
Niu, Li
Bai, Mengxuan
Song, Hongrui
Zhang, Lijuan
author_facet Ding, Huaiwei
Chen, Kai
Song, Bingke
Deng, Chenglong
Li, Wei
Niu, Li
Bai, Mengxuan
Song, Hongrui
Zhang, Lijuan
author_sort Ding, Huaiwei
collection PubMed
description Two series of benzamides compounds bearing piperidine groups were synthesized and the Gli-luc luciferase activity was screened by Gys-luc luciferase gene detection method. Compound 5q showed promising inhibition of hedgehog (Hh) signaling pathway. To further verify whether the Hh inhibitory activities of the target compounds are derived from their inhibition to the Smoothened (Smo) receptor, the compounds with good potency were evaluated in a fluorescence competitive displacement assays, the results showed the Smo inhibitory potency of these compounds correlated well with their Hh inhibition, which suggested that the observed Hh activity was driven by Smo inhibitors.
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spelling pubmed-60175362018-11-13 Synthesis and Smo Activity of Some Novel Benzamide Derivatives Ding, Huaiwei Chen, Kai Song, Bingke Deng, Chenglong Li, Wei Niu, Li Bai, Mengxuan Song, Hongrui Zhang, Lijuan Molecules Article Two series of benzamides compounds bearing piperidine groups were synthesized and the Gli-luc luciferase activity was screened by Gys-luc luciferase gene detection method. Compound 5q showed promising inhibition of hedgehog (Hh) signaling pathway. To further verify whether the Hh inhibitory activities of the target compounds are derived from their inhibition to the Smoothened (Smo) receptor, the compounds with good potency were evaluated in a fluorescence competitive displacement assays, the results showed the Smo inhibitory potency of these compounds correlated well with their Hh inhibition, which suggested that the observed Hh activity was driven by Smo inhibitors. MDPI 2017-12-31 /pmc/articles/PMC6017536/ /pubmed/29301237 http://dx.doi.org/10.3390/molecules23010085 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Ding, Huaiwei
Chen, Kai
Song, Bingke
Deng, Chenglong
Li, Wei
Niu, Li
Bai, Mengxuan
Song, Hongrui
Zhang, Lijuan
Synthesis and Smo Activity of Some Novel Benzamide Derivatives
title Synthesis and Smo Activity of Some Novel Benzamide Derivatives
title_full Synthesis and Smo Activity of Some Novel Benzamide Derivatives
title_fullStr Synthesis and Smo Activity of Some Novel Benzamide Derivatives
title_full_unstemmed Synthesis and Smo Activity of Some Novel Benzamide Derivatives
title_short Synthesis and Smo Activity of Some Novel Benzamide Derivatives
title_sort synthesis and smo activity of some novel benzamide derivatives
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017536/
https://www.ncbi.nlm.nih.gov/pubmed/29301237
http://dx.doi.org/10.3390/molecules23010085
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