Cytotoxic Assessment of 3,3-Dichloro-β-Lactams Prepared through Microwave-Assisted Benzylic C-H Activation from Benzyl-Tethered Trichloroacetamides Catalyzed by RuCl2(PPh3)3

• Published in: Molecules (Basel, Switzerland) Vol. 27; no. 18; p. 5975
• Main Authors: Diaba, Faïza, Sandor, Alexandra G., Morán, María del Carmen
• Format: Journal Article
• Language: English
• Published: Basel MDPI AG 14.09.2022; MDPI
• Subjects: 3,3-dichloro-β-lactams; A431 cell line; Amides; Antibiotics; Antidiabetics; Biological activity; C-H activation; Cancer; cytotoxic activity; Cytotoxicity; Diabetes mellitus; hemocompatibility; Hydrocarbons; Investigations; Metabolism; Selectivity; Skin; Squamous cell carcinoma; Tumor cells; β-Lactam antibiotics
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules27185975

Natural and synthetic β-lactam derivatives constitute an interesting class of compounds due to their diverse biological activity. Mostly used as antibiotics, they were also found to have antitubercular, anticancer and antidiabetic activities, among others. In this investigation, six new 3,3-dichloro-β-lactams prepared in a previous work were evaluated for their hemolytic and cytotoxic properties. The results showed that the proposed compounds have non-hemolytic properties and exhibited an interesting cytotoxic activity toward squamous cell carcinoma (A431 cell line), which was highly dependent on the structure and concentration of these β-lactams. Among the molecules tested, 2b was the most cytotoxic, with the lowest IC50 values (30–47 µg/mL) and a promising selectivity against the tumor cells compared with non-tumoral cells.