Bioorganic & medicinal chemistry letters, 2012-09, Vol.22 (17), p.5466-5469
2012
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- Autor(en) / Beteiligte
- Titel
- 2-Amino-1,3,4-thiadiazole derivative (FABT) inhibits the extracellular signal-regulated kinase pathway and induces cell cycle arrest in human non-small lung carcinoma cells
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2012-09, Vol.22 (17), p.5466-5469
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2012
- Quelle
- Elsevier ScienceDirect Journals
- Beschreibungen/Notizen
- The anticancer potential of 2-amino-1,3,4-thiadiazole compounds has been documented by in vitro and in vivo studies. In our previous research, we described the synthesis as well as the antiproliferative and neuroprotective activities of 2-(4-fluorophenyloamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole (FABT). The aim of the present study was to investigate the molecular mechanisms involved in FABT-induced growth inhibition in A549 lung carcinoma cells. Western blotting analysis revealed that FABT inhibited the activation of the extracellular signal-regulated kinase 1/2 (ERK1/2) pathway, and Real-time PCR analysis showed no changes in the expression of P44ERK1 and CREB1 genes. Furthermore, FABT induced cell cycle arrest in the GO/G1 phase and enhanced p27/Kip1 expression. Our results suggest that FABT acts by inhibiting ERK1/2 pathway and cell cycle progression through G1 into S phase in A549 cells. Further studies are needed to completely explain the molecular mechanisms of anticancer action of this 2-aminothiadiazole derivative.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2012.07.036Titel-ID: cdi_proquest_miscellaneous_1038599243
- Format
- –
- Schlagworte
- 2-Amino-1,3,4-thiadiazole, Anticancer activity, Antineoplastic Agents - chemistry, Antineoplastic Agents - pharmacology, Biological and medical sciences, Carcinoma, Non-Small-Cell Lung - drug therapy, Carcinoma, Non-Small-Cell Lung - enzymology, Carcinoma, Non-Small-Cell Lung - genetics, Carcinoma, Non-Small-Cell Lung - metabolism, Cell cycle, Cell cycle arrest, Cell Cycle Checkpoints - drug effects, Cell Line, Tumor, chemistry, Cyclin-dependent kinase inhibitor p27, Cyclin-Dependent Kinase Inhibitor p27 - genetics, ERK1/2 pathway, Extracellular signal-regulated kinase, Extracellular Signal-Regulated MAP Kinases - metabolism, G1 phase, Gene Expression Regulation, Neoplastic - drug effects, genes, growth retardation, Humans, in vivo studies, interphase, Lung carcinoma, lung neoplasms, Lung Neoplasms - drug therapy, Lung Neoplasms - enzymology, Lung Neoplasms - genetics, Lung Neoplasms - metabolism, MAP Kinase Signaling System - drug effects, Medical sciences, mitogen-activated protein kinase, Models, Molecular, Molecular modelling, Neuroprotection, neuroprotective effect, Non-small lung carcinoma, p27/Kip1, Pharmacology. Drug treatments, Polymerase chain reaction, quantitative polymerase chain reaction, S phase, Thiadiazoles - chemistry, Thiadiazoles - pharmacology, Western blotting