New chroman-4-one/thiochroman-4-one derivatives as potential anticancer agents

Abstract

The synthesis of 3-[3/4-(2-aryl-2-oxoethoxy)arylidene]chroman/thiochroman-4-one derivatives (-) and evaluation of their anticancer activities were aimed in this work. Final compounds were obtained in multistep synthesis reactions using phenol/thiophenol derivatives as starting materials. For anticancer activity evaluation, all compounds were offered to National Cancer Institute (NCI), USA and selected ones were tested against sixty human tumor cell lines derived from nine neoplastic diseases. The activity results were evaluated according to the drug screening protocol of the institute. Compounds containing thiochromanone skeleton exhibited higher anticancer activity.

Interaction of Arylidenechromanone/Flavanone Derivatives with Biological Macromolecules Studied as Human Serum Albumin Binding, Cytotoxic Effect, Biocompatibility Towards Red Blood Cells

“…For instance, it was found that, in vivo, quercetin exerts a chemo-preventive effect on prostate cancer (reduces the cell viability) by downregulating the activity of pro-proliferative and anti-apoptotic proteins [6]. Additionally, synthetic derivatives of naturally occurring flavonoids (e.g., derivatives of chroman-4-one and tiochromane-4-one [7]) are studied for their anti-cancer properties.…”

Synthetic Approaches to 2‐Alkylthiochroman‐4‐ones and Thioflavanones

“…Compound 6 was then heated with PPA to obtain the thiochroman‐4‐one derivatives ( 1 ) (Scheme 4). 19 …”

Fusing privileged structures: synthesis and characterization of new benzothiophene-chalcone hybrids

“…Chalcone can be regarded as a privileged structure as it is found in many natural and synthetic compounds featuring a wide range of biological activities, including antimicrobial, antitumor, antioxidant, anti-inflammatory, anticonvulsant, anti-estrogenic and anticancer, etc. 3 The chalcones' decreasing effect on free-radical formation may reduce DNA damage and the risk of mutagenicity. Also, most of the studies reported that chalcones induced apoptosis in the cancer-cell lines.…”

“…Also, most of the studies reported that chalcones induced apoptosis in the cancer-cell lines. [3][4] This significant substructure possesses a pharmacophoric effect along with anticancer activity described in many studies. [5][6] Although estrogen is primarily known as a reproductive hormone, it also displays many positive effects on the skeleton, cardiovascular and nervous systems.…”