Next Article in Journal
Heteroaromatic N-Oxides in Asymmetric Catalysis: A Review
Previous Article in Journal
The Generation of the Oxidant Agent of a Mononuclear Nonheme Fe(II) Biomimetic Complex by Oxidative Decarboxylation. A DFT Investigation
Previous Article in Special Issue
The Role of c-Met as a Biomarker and Player in Innate and Acquired Resistance in Non-Small-Cell Lung Cancer: Two New Mutations Warrant Further Studies
Open AccessArticle

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

1
Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy
2
Department of Medical Oncology, VU University Medical Center, Cancer Center Amsterdam, DeBoelelaan 1117, 1081HV Amsterdam, The Netherlands
3
Fondazione RI.MED, Via Bandiera 11, 90133 Palermo, Italy
4
Cancer Pharmacology Lab, Fondazione Pisana per la Scienza, via Ferruccio Giovannini 13, 56017 San Giuliano Terme, Pisa, Italy
*
Authors to whom correspondence should be addressed.
Equally contributed.
Academic Editors: Elisa Giovannetti and Patrizia Diana
Molecules 2020, 25(2), 329; https://doi.org/10.3390/molecules25020329 (registering DOI)
Received: 15 November 2019 / Revised: 23 December 2019 / Accepted: 28 December 2019 / Published: 14 January 2020
(This article belongs to the Special Issue Drug Resistance in Targeted Cancer Therapy)
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. View Full-Text
Keywords: imidazo[2,1-b][1,3,4]thiadiazole derivatives; antiproliferative activity; migration assay; indole compounds; pancreatic cancer; resistance imidazo[2,1-b][1,3,4]thiadiazole derivatives; antiproliferative activity; migration assay; indole compounds; pancreatic cancer; resistance
Show Figures

Graphical abstract

MDPI and ACS Style

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. 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 2020, 25, 329.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop