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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Main Authors:	Huaiwei Ding, Kai Chen, Bingke Song, Chenglong Deng, Wei Li, Li Niu, Mengxuan Bai, Hongrui Song, Lijuan Zhang
Format:	Article
Language:	English
Published:	MDPI AG 2017-12-01
Series:	Molecules
Subjects:	benzamide hedgehog signaling Gli-luc luciferase activity
Online Access:	https://www.mdpi.com/1420-3049/23/1/85

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spelling	doaj-2ee7894d254f42f588fd3a757bd11e932020-11-25T00:35:54ZengMDPI AGMolecules1420-30492017-12-012318510.3390/molecules23010085molecules23010085Synthesis and Smo Activity of Some Novel Benzamide DerivativesHuaiwei Ding0Kai Chen1Bingke Song2Chenglong Deng3Wei Li4Li Niu5Mengxuan Bai6Hongrui Song7Lijuan Zhang8Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, ChinaKey Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, ChinaKey Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, ChinaKey Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, ChinaKey Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, ChinaKey Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, ChinaKey Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, ChinaKey Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, ChinaKey Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, ChinaTwo 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.https://www.mdpi.com/1420-3049/23/1/85benzamidehedgehog signalingGli-luc luciferase activity
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Huaiwei Ding Kai Chen Bingke Song Chenglong Deng Wei Li Li Niu Mengxuan Bai Hongrui Song Lijuan Zhang
spellingShingle	Huaiwei Ding Kai Chen Bingke Song Chenglong Deng Wei Li Li Niu Mengxuan Bai Hongrui Song Lijuan Zhang Synthesis and Smo Activity of Some Novel Benzamide Derivatives Molecules benzamide hedgehog signaling Gli-luc luciferase activity
author_facet	Huaiwei Ding Kai Chen Bingke Song Chenglong Deng Wei Li Li Niu Mengxuan Bai Hongrui Song Lijuan Zhang
author_sort	Huaiwei Ding
title	Synthesis and Smo Activity of Some Novel Benzamide Derivatives
title_short	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_sort	synthesis and smo activity of some novel benzamide derivatives
publisher	MDPI AG
series	Molecules
issn	1420-3049
publishDate	2017-12-01
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.
topic	benzamide hedgehog signaling Gli-luc luciferase activity
url	https://www.mdpi.com/1420-3049/23/1/85
work_keys_str_mv	AT huaiweiding synthesisandsmoactivityofsomenovelbenzamidederivatives AT kaichen synthesisandsmoactivityofsomenovelbenzamidederivatives AT bingkesong synthesisandsmoactivityofsomenovelbenzamidederivatives AT chenglongdeng synthesisandsmoactivityofsomenovelbenzamidederivatives AT weili synthesisandsmoactivityofsomenovelbenzamidederivatives AT liniu synthesisandsmoactivityofsomenovelbenzamidederivatives AT mengxuanbai synthesisandsmoactivityofsomenovelbenzamidederivatives AT hongruisong synthesisandsmoactivityofsomenovelbenzamidederivatives AT lijuanzhang synthesisandsmoactivityofsomenovelbenzamidederivatives
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Synthesis and Smo Activity of Some Novel Benzamide Derivatives

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