3-(6-Phenylimidazo [2,1-b][1,3,4]thiadiazol-2-yl)-1H-Indole Derivatives as New Anticancer Agents in the Treatment of Pancreatic Ductal Adenocarcinoma
| Autor: | Daniela Carbone, Godefridus J. Peters, Ugo Perricone, Elisa Giovannetti, Btissame El Hassouni, Girolamo Cirrincione, Giovanna Li Petri, Barbara Parrino, Stella Cascioferro, Vincenzo Arizza, Patrizia Diana, Niccola Funel, Alessandro Padova |
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| Přispěvatelé: | Medical oncology laboratory, AGEM - Re-generation and cancer of the digestive system, CCA - Cancer biology and immunology, Cascioferro S., Li Petri G., Parrino B., El Hassouni B., Carbone D., Arizza V., Perricone U., Padova A., Funel N., Peters G.J., Cirrincione G., Giovannetti E., Diana P. |
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
antiproliferative activity
Pancreatic ductal adenocarcinoma endocrine system diseases pancreatic cancer Pharmaceutical Science Imidazo[2 1-b][1 3 4]thiadiazole derivative Analytical Chemistry resistance lcsh:QD241-441 03 medical and health sciences 0302 clinical medicine lcsh:Organic chemistry Pancreatic cancer Drug Discovery medicine Physical and Theoretical Chemistry IC50 imidazo[2 1-b][1 3 4]thiadiazole derivatives 030304 developmental biology Indole test 0303 health sciences migration assay Migration Assay Chemistry Organic Chemistry Biological activity indole compounds medicine.disease In vitro digestive system diseases Indole compound Chemistry (miscellaneous) Cell culture 030220 oncology & carcinogenesis Cancer research Molecular Medicine |
| Zdroj: | Molecules, 25(2):329. Multidisciplinary Digital Publishing Institute Molecules, Vol 25, Iss 2, p 329 (2020) Molecules Volume 25 Issue 2 Cascioferro, S, Li Petri, G, Parrino, B, el Hassouni, B, Carbone, D, Arizza, V, Perricone, U, Padova, A, Funel, N, Peters, G J, Cirrincione, G, Giovannetti, E & Diana, P 2020, ' 3-(6-Phenylimidazo [2,1-b][1,3,4]thiadiazol-2-yl)-1H-Indole Derivatives as New Anticancer Agents in the Treatment of Pancreatic Ductal Adenocarcinoma ', Molecules, vol. 25, no. 2, 329 . https://doi.org/10.3390/molecules25020329 |
| ISSN: | 1420-3049 |
| DOI: | 10.3390/molecules25020329 |
| Popis: | A new series of imidazo[2,1-b][1,3,4]thiadiazole derivatives was efficiently synthesized and screened for their in vitro antiproliferative activity on a panel of pancreatic ductal adenocarcinoma (PDAC) cells, including SUIT-2, Capan-1 and Panc-1. Compounds 9c and 9l, showed relevant in vitro antiproliferative activity on all three pre-clinical models with half maximal inhibitory concentration (IC50) ranging from 5.11 to 10.8 µ M, while the compounds 9e and 9n were active in at least one cell line. In addition, compound 9c significantly inhibited the migration rate of SUIT-2 and Capan-1 cells in the scratch wound-healing assay. In conclusion, our results will support further studies to increase the library of imidazo [2,1-b][1,3,4] thiadiazole derivatives for deeper understanding of the relationship between biological activity of the compounds and their structures in the development of new antitumor compounds against pancreatic diseases. |
| Databáze: | OpenAIRE |
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