A Structure-Activity Relationship Study of Amino Acid Derivatives of Pterostilbene Analogues Toward Human Breast Cancer

ChemMedChem. 2024 Feb 12:e202300727. doi: 10.1002/cmdc.202300727. Online ahead of print.ABSTRACTPterostilbene is the dimethylated analogue of Resveratrol, a compound with well-known biological activities, such as antioxidant, chemopreventive, anti-diabetic, anti-obesity, and cardioprotective. Despite many studies on the general effect of such polyphenolic molecules and their derivatives, a deep comprehension of their action and systematic structure-activity relationship studies are still rare. Herein, three different analogues of functionalizable Pterostilbene were efficiently synthesized and derivatized with a selected library of antioxidant amino acids, allowing for a highly diversified exploration of the chemical space. The library was analyzed towards cancer cells. Collectively, our data demonstrated the enhanced anti-proliferative activity of Tryptophan-conjugated compounds. In breast cancer cells, the treatment with Tryptophan-conjugated analogues induced the activation of cellular stress pathways, including autophagy signaling.PMID:38346281 | DOI:10.1002/cmdc.202300727
Source: ChemMedChem - Category: Chemistry Authors: Source Type: research