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Novel thiazolidines of potential anti-proliferation properties against esophageal squamous cell carcinoma via ERK pathway.
Aziz, Marian N; Nguyen, Linh; Chang, Yan; Gout, Delphine; Pan, Zui; Lovely, Carl J.
Afiliación
  • Aziz MN; Department of Chemistry and Biochemistry, 700 Planetarium Place, University of Texas at Arlington, TX, 76019, USA; Department of Pesticide Chemistry, National Research Centre, Dokki, Giza, 12622, Egypt.
  • Nguyen L; Dept. of Biology, College of Science, University of Texas at Arlington, TX, 76019, USA; Department of Graduate Nursing, College of Nursing and Health Innovation, University of Texas at Arlington, TX, 76019, USA.
  • Chang Y; Department of Graduate Nursing, College of Nursing and Health Innovation, University of Texas at Arlington, TX, 76019, USA; Bone and Muscle Research Center, University of Texas at Arlington, TX, 76019, USA.
  • Gout D; Department of Chemistry and Biochemistry, 700 Planetarium Place, University of Texas at Arlington, TX, 76019, USA.
  • Pan Z; Department of Graduate Nursing, College of Nursing and Health Innovation, University of Texas at Arlington, TX, 76019, USA; Bone and Muscle Research Center, University of Texas at Arlington, TX, 76019, USA.
  • Lovely CJ; Department of Chemistry and Biochemistry, 700 Planetarium Place, University of Texas at Arlington, TX, 76019, USA. Electronic address: lovely@uta.edu.
Eur J Med Chem ; 246: 114909, 2023 Jan 15.
Article en En | MEDLINE | ID: mdl-36508971
The discovery of a new class of extracellular-signal-regulated kinase (ERK) inhibitors has been achieved via developing novel 2-imino-5-arylidene-thiazolidine analogues. A novel synthetic method employing a solid support-mediated reaction was used to construct the targeted thiazolidines through a cascade reaction with good yields. The chemical and physical stability of the new thiazolidine library has successfully been achieved by blocking the labile C5-position to aerobic oxidation. A cell viability study was performed using esophageal squamous cell carcinoma cell lines (KYSE-30 and KYSE-150) and non-tumorous esophageal epithelial cell lines (HET-1A and NES-G4T) through utilization of an MTT assay, revealing that (Z)-5-((Z)-4-bromobenzylidene)-N-(4-methoxy-2-nitrophenyl)-4,4-dimethylthiazolidin-2-imine (6g) was the best compound among the synthesized library in terms of selectivity. DAPI staining experiments were performed to visualize the morphological changes and to investigate the apoptotic activity. Moreover, western blots were used to probe the mechanism/pathway behind the observed activity/selectivity of thiazolidine 6g which established selective inhibition of phosphorylation in the ERK pathway. Molecular modeling techniques have been utilized to confirm the observed activity. A molecular docking study revealed similar binding interactions between the synthesized thiazolidines and reported co-crystalized inhibitors with ERK proteins. Thus, the present study provides a starting point for the development of interesting bioactive 2-imino-5-arylidene-thiazolidines.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Neoplasias Esofágicas / Carcinoma de Células Escamosas de Esófago Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2023 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Francia
Texto completo
Añadir a Mi BVS
Imprimir
XML
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Neoplasias Esofágicas / Carcinoma de Células Escamosas de Esófago Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2023 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Francia