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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

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 antipro...

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Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7024338/
https://www.ncbi.nlm.nih.gov/pubmed/31947550
http://dx.doi.org/10.3390/molecules25020329
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author 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
author_facet 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
author_sort Cascioferro, Stella
collection PubMed
description 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 (IC(50)) 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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spelling pubmed-70243382020-03-11 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 Molecules Article 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 (IC(50)) 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. MDPI 2020-01-14 /pmc/articles/PMC7024338/ /pubmed/31947550 http://dx.doi.org/10.3390/molecules25020329 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
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
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
title_full 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
title_fullStr 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
title_full_unstemmed 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
title_short 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
title_sort 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
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7024338/
https://www.ncbi.nlm.nih.gov/pubmed/31947550
http://dx.doi.org/10.3390/molecules25020329
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