Artículo
Benzothiazole Derivatives Endowed with Antiproliferative Activity in Paraganglioma and Pancreatic Cancer Cells: Structure–Activity Relationship Studies and Target Prediction Analysis
Autor/es | Amoroso, Rosa
De Lellis, Laura Florio, Rosalba Moreno Rodríguez, Nazaret Agamennone, Mariangela De Filippis, Barbara Giampietro, Letizia Maccallini, Cristina Fernández Fernández, Inmaculada Recio Jiménez, Rocío Cama, Alessandro Fantacuzzi, Marialuigia Ammazzalorso, Alessandra |
Departamento | Universidad de Sevilla. Departamento de Química Orgánica y Farmacéutica |
Fecha de publicación | 2022 |
Fecha de depósito | 2022-09-16 |
Publicado en |
|
Resumen | The antiproliferative effects played by benzothiazoles in different cancers have aroused the interest for these molecules as promising antitumor agents. In this work, a library of phenylacetamide derivatives containing the ... The antiproliferative effects played by benzothiazoles in different cancers have aroused the interest for these molecules as promising antitumor agents. In this work, a library of phenylacetamide derivatives containing the benzothiazole nucleus was synthesized and compounds were tested for their antiproliferative activity in paraganglioma and pancreatic cancer cell lines. The novel synthesized compounds induced a marked viability reduction at low micromolar concentrations both in paraganglioma and pancreatic cancer cells. Derivative 4l showed a greater antiproliferative effect and higher selectivity index against cancer cells, as compared to other compounds. Notably, combinations of derivative 4l with gemcitabine at low concentrations induced enhanced and synergistic effects on pancreatic cancer cell viability, thus supporting the relevance of compound 4l in the perspective of clinical translation. A target prediction analysis was also carried out on 4l by using multiple computational tools, identifying cannabinoid receptors and sentrin-specific proteases as putative targets contributing to the observed antiproliferative activity. |
Agencias financiadoras | Ministero dell’Istruzione, dell’Università e della Ricerca |
Identificador del proyecto | PRIN 2017EKMFTN_005 |
Cita | Amoroso, R., De Lellis, L., Florio, R., Moreno Rodríguez, N., Agamennone, M., De Filippis, B.,...,Ammazzalorso, A. (2022). Benzothiazole Derivatives Endowed with Antiproliferative Activity in Paraganglioma and Pancreatic Cancer Cells: Structure–Activity Relationship Studies and Target Prediction Analysis. Pharmaceuticals, 15 (8), 937. |
Ficheros | Tamaño | Formato | Ver | Descripción |
---|---|---|---|---|
Benzothiazole Derivatives.pdf | 1.983Mb | [PDF] | Ver/ | |