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

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

Research output: Contribution to journalArticleAcademicpeer-review

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 languageEnglish
Article numberE329
JournalMolecules
Volume25
Issue number2
DOIs
Publication statusPublished - 2020

Cite this

Cascioferro, Stella ; Li Petri, Giovanna ; Parrino, Barbara ; el Hassouni, Btissame ; Carbone, Daniela ; Arizza, Vincenzo ; Perricone, Ugo ; Padova, Alessandro ; Funel, Niccola ; Peters, Godefridus J. ; Cirrincione, Girolamo ; Giovannetti, Elisa ; Diana, Patrizia. / 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. In: Molecules. 2020 ; Vol. 25, No. 2.
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title = "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",
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.",
keywords = "Antiproliferative activity, Imidazo[2,1-b][1,3,4]thiadiazole derivatives, Indole compounds, Migration assay, Pancreatic cancer, Resistance",
author = "Stella Cascioferro and {Li Petri}, Giovanna and Barbara Parrino and {el Hassouni}, Btissame and Daniela Carbone and Vincenzo Arizza and Ugo Perricone and Alessandro Padova and Niccola Funel and Peters, {Godefridus J.} and Girolamo Cirrincione and Elisa Giovannetti and Patrizia Diana",
year = "2020",
doi = "10.3390/molecules25020329",
language = "English",
volume = "25",
journal = "Molecules",
issn = "1420-3049",
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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. / Cascioferro, Stella; Li Petri, Giovanna; Parrino, Barbara; el Hassouni, Btissame; Carbone, Daniela; Arizza, Vincenzo; Perricone, Ugo; Padova, Alessandro; Funel, Niccola; Peters, Godefridus J.; Cirrincione, Girolamo; Giovannetti, Elisa; Diana, Patrizia.

In: Molecules, Vol. 25, No. 2, E329, 2020.

Research output: Contribution to journalArticleAcademicpeer-review

TY - JOUR

T1 - 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

AU - Cascioferro, Stella

AU - Li Petri, Giovanna

AU - Parrino, Barbara

AU - el Hassouni, Btissame

AU - Carbone, Daniela

AU - Arizza, Vincenzo

AU - Perricone, Ugo

AU - Padova, Alessandro

AU - Funel, Niccola

AU - Peters, Godefridus J.

AU - Cirrincione, Girolamo

AU - Giovannetti, Elisa

AU - Diana, Patrizia

PY - 2020

Y1 - 2020

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 - Imidazo[2,1-b][1,3,4]thiadiazole derivatives

KW - Indole compounds

KW - Migration assay

KW - Pancreatic cancer

KW - Resistance

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UR - https://www.ncbi.nlm.nih.gov/pubmed/31947550

U2 - 10.3390/molecules25020329

DO - 10.3390/molecules25020329

M3 - Article

VL - 25

JO - Molecules

JF - Molecules

SN - 1420-3049

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ER -