Synthesis and anti-cancer activity evaluation of new aurone derivatives

Abstract

In this study, we have synthesized 2-[3-or 4-(2-aryl-2-oxoethoxy)arylidene]benzofuran-3-one derivatives (D1-D38) and evaluated their anti-cancer activities. The final compounds were obtained in multistep synthesis reactions using benzofuranon-3-one derivatives (A1-A4, B) as starting materials which were gained in various synthetic ways. Aurone derivatives (C1-C10) were acquired with the condensation reaction of these starting materials and 3-/4-hydroxybenzaldehyde which were then reacted with a-bromoacetophenones to get final compounds. The anti-cancer activity of the selected compounds was performed by National Cancer Institute (NCI), USA against 60 human tumor cell lines derived from nine neoplastic diseases. Compounds exhibited anti-cancer activity in varying ratios.

Auronidins are a previously unreported class of flavonoid pigments that challenges when anthocyanin biosynthesis evolved in plants

“…SI Appendix, Table S1 provides the chemical shift values for the proton and carbon atoms. D) at wavelengths that may provide opportunities for new chemistry-based practical applications, for example, as chemosensors in dye-sensitized solar cells (26) or in the base compound of a line of pharmaceutical derivatives (27).…”

Synthesis and Biological Evaluation of Quinoline‐Based Novel Aurones

“…Plant uses aurones as phytoalexin, which acts as defendant counter to numerous infections . In recent past, aurones have earned attention of medicinal chemists because of their immense range of biological accent like antioxidant, antifungal, thyrosinase inhibition, antiparasitic, anticancer, antileishmanial activities. Some of the well‐known aurones are Aureusidin, Sulfuretin and Hemiltron, where aureusidin prohibit iodothyronine deiodinase, sulfuretin displays antiradical activity and hemiltron is known for its DNA strand scission activity Figure .…”

Exploring Aurone Derivatives as Potential Human Pancreatic Lipase Inhibitors through Molecular Docking and Molecular Dynamics Simulations

“…They are also considered phytoalexins produced by plants in response to pathogen attack [ 33 ]. Aurone derivatives have been reported to possess different bio-activities [ 34 ], such as anti-inflammatory [ 35 ], antibacterial [ 36 ], anti-malarial [ 37 , 38 ], anti-hepatitis [ 39 , 40 ], antioxidant [ 41 , 42 , 43 , 44 ], anticancer [ 45 , 46 , 47 , 48 , 49 ], and others. However, their ability to inhibit HPL has not been studied.…”