3-(6-Phenylimidazo [2,1-b][1,3,4]thiadiazol-2-yl)-1HIndole derivatives as new anticancer agents in the treatment of pancreatic ductal adenocarcinoma

Girolamo Cirrincione; Barbara Parrino; Patrizia Diana; Vincenzo Arizza; Stella Maria Cascioferro; Giovanna Li Petri; Daniela Carbone; Godefridus J. Peters; Ugo Perricone; Btissame El Hassouni; Giovanna Li Petri; Niccola Funel; Alessandro Padova; Elisa Giovannetti

3-(6-Phenylimidazo [2,1-b][1,3,4]thiadiazol-2-yl)-1HIndole derivatives as new anticancer agents in the treatment of pancreatic ductal adenocarcinoma

Girolamo Cirrincione, Barbara Parrino, Patrizia Diana, Vincenzo Arizza, Stella Maria Cascioferro, Giovanna Li Petri, Daniela Carbone, Godefridus J. Peters, Ugo Perricone, Btissame El Hassouni, Giovanna Li Petri, Niccola Funel, Alessandro Padova, Elisa Giovannetti

Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche

Research output: Contribution to journal › Article › peer-review

8 Citations (Scopus)

Abstract

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 μM, 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.

Original language	English
Pages (from-to)	1-16
Number of pages	16
Journal	Molecules
Volume	25
Publication status	Published - 2020

All Science Journal Classification (ASJC) codes

Analytical Chemistry
Chemistry (miscellaneous)
Molecular Medicine
Pharmaceutical Science
Drug Discovery
Physical and Theoretical Chemistry
Organic Chemistry

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Cirrincione, G., Parrino, B., Diana, P., Arizza, V., Cascioferro, S. M., Li Petri, G., Carbone, D., Peters, G. J., Perricone, U., El Hassouni, B., Petri, G. L., Funel, N., Padova, A., & Giovannetti, E. (2020). 3-(6-Phenylimidazo [2,1-b][1,3,4]thiadiazol-2-yl)-1HIndole derivatives as new anticancer agents in the treatment of pancreatic ductal adenocarcinoma. Molecules, 25, 1-16.

3-(6-Phenylimidazo [2,1-b][1,3,4]thiadiazol-2-yl)-1HIndole derivatives as new anticancer agents in the treatment of pancreatic ductal adenocarcinoma. / Cirrincione, Girolamo ; Parrino, Barbara ; Diana, Patrizia ; Arizza, Vincenzo ; Cascioferro, Stella Maria ; Li Petri, Giovanna ; Carbone, Daniela; Peters, Godefridus J.; Perricone, Ugo; El Hassouni, Btissame; Petri, Giovanna Li; Funel, Niccola; Padova, Alessandro; Giovannetti, Elisa.

In: Molecules, Vol. 25, 2020, p. 1-16.

Research output: Contribution to journal › Article › peer-review

Cirrincione, Girolamo ; Parrino, Barbara ; Diana, Patrizia ; Arizza, Vincenzo ; Cascioferro, Stella Maria ; Li Petri, Giovanna ; Carbone, Daniela ; Peters, Godefridus J. ; Perricone, Ugo ; El Hassouni, Btissame ; Petri, Giovanna Li ; Funel, Niccola ; Padova, Alessandro ; Giovannetti, Elisa. / 3-(6-Phenylimidazo [2,1-b][1,3,4]thiadiazol-2-yl)-1HIndole derivatives as new anticancer agents in the treatment of pancreatic ductal adenocarcinoma. In: Molecules. 2020 ; Vol. 25. pp. 1-16.

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title = "3-(6-Phenylimidazo [2,1-b][1,3,4]thiadiazol-2-yl)-1HIndole derivatives as new anticancer agents in the treatment of pancreatic ductal adenocarcinoma",

abstract = "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 μM, 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.",

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author = "Girolamo Cirrincione and Barbara Parrino and Patrizia Diana and Vincenzo Arizza and Cascioferro, {Stella Maria} and {Li Petri}, Giovanna and Daniela Carbone and Peters, {Godefridus J.} and Ugo Perricone and {El Hassouni}, Btissame and Petri, {Giovanna Li} and Niccola Funel and Alessandro Padova and Elisa Giovannetti",

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T1 - 3-(6-Phenylimidazo [2,1-b][1,3,4]thiadiazol-2-yl)-1HIndole derivatives as new anticancer agents in the treatment of pancreatic ductal adenocarcinoma

AU - Cirrincione, Girolamo

AU - Parrino, Barbara

AU - Diana, Patrizia

AU - Arizza, Vincenzo

AU - Cascioferro, Stella Maria

AU - Li Petri, Giovanna

AU - Carbone, Daniela

AU - Peters, Godefridus J.

AU - Perricone, Ugo

AU - El Hassouni, Btissame

AU - Petri, Giovanna Li

AU - Funel, Niccola

AU - Padova, Alessandro

AU - Giovannetti, Elisa

PY - 2020

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N2 - 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 μM, 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.

AB - 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 μM, 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.

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KW - 1-b][1

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KW - 4]thiadiazole derivatives; Indole compounds; Migration assay; Pancreatic cancer; Resistance

KW - Antiproliferative activity; Imidazo[2

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