Next Article in Journal
Characterization of Vasorelaxant Principles from the Needles of Pinus morrisonicola Hayata
Previous Article in Journal
A Polarizable Atomic Multipole-Based Force Field for Molecular Dynamics Simulations of Anionic Lipids
Article Menu
Issue 1 (January) cover image

Export Article

Open AccessArticle
Molecules 2018, 23(1), 85; https://doi.org/10.3390/molecules23010085

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]   |  

Abstract

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
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Supplementary material

SciFeed

Share & Cite This Article

MDPI and ACS Style

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.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top