2. Academic Validation
  3. Synthesis and Smo Activity of Some Novel Benzamide Derivatives

Synthesis and Smo Activity of Some Novel Benzamide Derivatives

  • Molecules. 2017 Dec 31;23(1):85. doi: 10.3390/molecules23010085.
Huaiwei Ding 1,  Kai Chen 2,  Bingke Song 3,  Chenglong Deng 4,  Wei Li 5,  Li Niu 6,  Mengxuan Bai 7,  Hongrui Song 8,  Lijuan Zhang 9
Affiliations

Affiliations

  • 1 Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. [email protected].
  • 2 Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. [email protected].
  • 3 Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. [email protected].
  • 4 Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. [email protected].
  • 5 Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. [email protected].
  • 6 Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. [email protected].
  • 7 Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. [email protected].
  • 8 Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. [email protected].
  • 9 Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. [email protected].
PMID: 29301237 DOI: 10.3390/molecules23010085
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.

Keywords

Gli-luc luciferase activity; benzamide; hedgehog signaling.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-12848
    99.79%, Smoothened Agonist
    Smo