Synthetic derivatives of natural cinnamic acids as potential anti-colorectal cancer agents

Falbo F, Gemma S, Koch AM, Mazzotta S, Carullo G, Ramunno A, Butini S, Schneider-Stock R, Campiani G, Aiello F (2024)

Publication Type: Journal article

Publication year: 2024

Journal

Chemical Biology & Drug Design Wiley-Blackwell

Book Volume: 103

Article Number: e14415

Journal Issue: 1

DOI: 10.1111/cbdd.14415

Abstract

Cinnamic acid and its derivatives represent attractive building blocks for the development of pharmacological tools. A series of piperoniloyl and cinnamoyl-based amides (6-9 a-f) have been synthesized and assayed against a wide panel of colorectal cancer (CRC) cells, with the aim of finding promising anticancer agents. Among all twenty-four synthesized molecules, 7a, 7e-f, 9c, and 9f displayed the best antiproliferative activity. The induced G1 cell cycle arrest and the increase in apoptotic cell death was seen in FACS analysis and western Blotting in the colon tumor cell lines HCT116, SW480, LoVo, and HT29, but not in the nontumor cell line HCEC. In particular, 9f overcame the resistance of HT29 cells, which have a mutant p53 and BRAF. Furthermore, 9f, amide of piperonilic acid with the 3,4-dichlorobenzyl substituent upregulated p21, which is involved in cell cycle arrest as well as in apoptosis induction. Cinnamic acid derivatives might be potential anticancer compounds, useful for the development of promising anti-CRC agents.

Authors with CRIS profile

Anna Maria Koch Department of Paediatric Cardiac Surgery Regine Schneider-Stock Professur für Experimentelle Tumorpathologie

Involved external institutions

Università della Calabria (UNICAL) IT Italy (IT) Università degli Studi di Siena (UNISI) / University of Siena IT Italy (IT) Università degli studi di Milano IT Italy (IT) Università degli Studi di Salerno IT Italy (IT)

How to cite

APA:

Falbo, F., Gemma, S., Koch, A.M., Mazzotta, S., Carullo, G., Ramunno, A.,... Aiello, F. (2024). Synthetic derivatives of natural cinnamic acids as potential anti-colorectal cancer agents. Chemical Biology & Drug Design, 103(1). https://doi.org/10.1111/cbdd.14415

MLA:

Falbo, Federica, et al. "Synthetic derivatives of natural cinnamic acids as potential anti-colorectal cancer agents." Chemical Biology & Drug Design 103.1 (2024).

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