New chalcone-type compounds and 2-pyrazoline derivatives: synthesis and caspase-dependent anticancer activity

• Type: Article in International Scientific Journal
• Date: 2020

Authors

Chouiter, MI (Author) Other; Boulebd, H (Author) Other; David M Pereira (Author) FFUP; Patricia Valentao (Author) FFUP; Paula B Andrade (Author) FFUP; Belfaitah, A (Author) Other; Silva, AMS (Author) Other

Journal

Title: Future Medicinal Chemistry

Vol. 12

Pages: 493-509

ISSN: 1756-8919

Publisher: Future Medicine Ltd.

Indexing

ISI Web of Knowledge - 0 Citations

Scopus - 8 Citations

Other information

Authenticus ID: P-00R-XNP

DOI: 10.4155/fmc-2019-0342

Abstract (EN): Aim: There is a continuous and urgent need for new anticancer agents with novel structures and target selectivity. Methods & results: The anticancer activity of the prepared compounds was assessed against human lung (A549) and stomach (AGS) cancer cell lines and evaluated in the noncancer human lung fibroblast (MRC-5) cell line. 2-Pyrazolines were devoid of toxicity in all cell lines used, chalcones bearing a beta-(benz)imidazole moiety being toxic toward AGS cell line. Mechanistic studies showed that these compounds trigger loss of cell viability and mitochondrial membrane potential, while eliciting morphological traits compatible with regulated cell death, which was ultimately shown to derive from caspase activation, specifically caspase-3. Conclusion: Chalcones 1-3 have been identified as new and promising anticancer agents toward the AGS cell line.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 17