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
N1 - Funding Information: This project was supported by a 2014-2020 PON Ricerca e Innovazione grant from the Italian Ministry of Education, University and Research, entitled PROGEMA-Processi Green per l'Estrazione di Principi Attivi e la Depurazione di Matrici di Scarto e Non (ARS01_00432) to P.D. and by the AIRC Start-up grant to E.G. Funding Information: Funding: This project was supported by a 2014–2020 PON Ricerca e Innovazione grant from the Italian Ministry of Education, University and Research, entitled “PROGEMA—Processi Green per l’Estrazione di Principi Attivi e la Depurazione di Matrici di Scarto e Non” (ARS01_00432) to P.D. and by the AIRC Start‐up grant to E.G. Publisher Copyright: © 2020 by the authors. Licensee MDPI, Basel, Switzerland. Copyright: Copyright 2020 Elsevier B.V., All rights reserved.
PY - 2020/1/14
Y1 - 2020/1/14
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.
KW - Antiproliferative activity
KW - Imidazo[2,1-b][1,3,4]thiadiazole derivatives
KW - Indole compounds
KW - Migration assay
KW - Pancreatic cancer
KW - Resistance
UR - http://www.scopus.com/inward/record.url?scp=85078002862&partnerID=8YFLogxK
U2 - https://doi.org/10.3390/molecules25020329
DO - https://doi.org/10.3390/molecules25020329
M3 - Article
C2 - 31947550
SN - 1420-3049
VL - 25
JO - Molecules
JF - Molecules
IS - 2
M1 - 329
ER -