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New Pharmacological Strategies against Pancreatic Adenocarcinoma: The Multifunctional Thiosemicarbazone FA4.
Anobile, Dario P; Niso, Mauro; Puerta, Adrian; Fraga Rodrigues, Stephanie M; Abatematteo, Francesca S; Avan, Amir; Abate, Carmen; Riganti, Chiara; Giovannetti, Elisa.
Afiliação
  • Anobile DP; Department of Oncology, University of Torino, Via Santena 5/bis, 10026 Torino, Italy.
  • Niso M; Department of Medical Oncology, Amsterdam UMC, VU University, Cancer Center Amsterdam, De Boelelaan 1117, 1081HV Amsterdam, The Netherlands.
  • Puerta A; Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari ALDO MORO, Via Orabona 4, 70125 Bari, Italy.
  • Fraga Rodrigues SM; Department of Medical Oncology, Amsterdam UMC, VU University, Cancer Center Amsterdam, De Boelelaan 1117, 1081HV Amsterdam, The Netherlands.
  • Abatematteo FS; BioLab, Instituto Universitario de Bio-Orgánica "Antonio González" (IUBO-AG), Universidad de La Laguna, c/Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain.
  • Avan A; Department of Medical Oncology, Amsterdam UMC, VU University, Cancer Center Amsterdam, De Boelelaan 1117, 1081HV Amsterdam, The Netherlands.
  • Abate C; Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari ALDO MORO, Via Orabona 4, 70125 Bari, Italy.
  • Riganti C; Basic Medical Sciences Institute, Mashhad University of Medical Science, Mashhad 91886-17871, Iran.
  • Giovannetti E; Metabolic Syndrome Research Center, Mashhad University of Medical Science, Mashhad 91886-17871, Iran.
Molecules ; 27(5)2022 Mar 04.
Article em En | MEDLINE | ID: mdl-35268783
A new sigma-2 (σ2) receptor ligand (FA4) was efficiently synthesized and evaluated for cytotoxic, proapoptotic, and antimigratory activity on pancreatic ductal adenocarcinoma (PDAC) primary cell cultures, which restrained the aggressive and chemoresistant behavior of PDAC. This compound showed relevant antiproliferative activity with half maximal inhibitory concentration (IC50) values ranging from 0.701 to 0.825 µM. The cytotoxic activity was associated with induction of apoptosis, resulting in apoptotic indexes higher than those observed after exposure to a clinically relevant concentration of the gemcitabine, the first-line drug used against PDAC. Interestingly, FA4 was also able to significantly inhibit the migration rate of both PDAC-1 and PDAC-2 cells in the scratch wound-healing assay. In conclusion, our results support further studies to improve the library of thiosemicarbazones targeting the σ-2 receptor for a deeper understanding of the relationship between the biological activity of these compounds and the development of more efficient anticancer compounds against PDAC.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias Pancreáticas Idioma: En Ano de publicação: 2022 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias Pancreáticas Idioma: En Ano de publicação: 2022 Tipo de documento: Article