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Molecules 2018, 23(1), 85;

Synthesis and Smo Activity of Some Novel Benzamide Derivatives

Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China
Authors to whom correspondence should be addressed.
Received: 24 November 2017 / Revised: 28 December 2017 / Accepted: 29 December 2017 / Published: 31 December 2017
(This article belongs to the Section Medicinal Chemistry)
Full-Text   |   PDF [2271 KB, uploaded 31 December 2017]   |  


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. View Full-Text
Keywords: benzamide; hedgehog signaling; Gli-luc luciferase activity benzamide; hedgehog signaling; Gli-luc luciferase activity

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Ding, H.; Chen, K.; Song, B.; Deng, C.; Li, W.; Niu, L.; Bai, M.; Song, H.; Zhang, L. Synthesis and Smo Activity of Some Novel Benzamide Derivatives. Molecules 2018, 23, 85.

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