Design and Synthesis of Novel Nonsteroidal Phytoestrogen‐based Probes as Potential Biomarker: Evaluation of Anticancer Activity and Docking Studies

Abstract

in Wiley Online Library (wileyonlinelibrary.com).Two series of novel flavones and flavone-tanaproget conjugates were designed, synthesized, 125 Iradiolabeled, and evaluated for their antiproliferative activity against human cancer cell lines (MCF-7, MDA-MB-231, and HeLa). They exhibited good-to-excellent in vitro antiproliferative activity. For improving the receptor-binding affinity of synthesized compounds, flavone-tanaproget moieties were linked together through alkyl-alkenyl chain spacer, and the butyl chain was substituted at C-3 position of oxa-and aza-flavones to enhance the lypophilicity of the molecule. These compounds are hypothesized to bind with estrogen and progesterone receptors by docking studies, and binding affinities were shown to increase significantly compared with the reference ligands.

Zinc oxide-decorated polypyrrole/chitosan bionanocomposites with enhanced photocatalytic, antibacterial and anticancer performance

“…The anticancer potential of the chitosan and polypyrrole-based bio-nanocomposite was determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay following a previous report. 33 MTT assay is a colorimetric assay, which is based on the ability to cleave the tetrazolium ring of the MTT by the mitochondrial dehydrogenase enzyme of viable cells to form insoluble formazan crystals, which deposit on the living cells. This insoluble formazan is then dissolved by the addition of a suitable solvent to form a purple coloured solution.…”

Three-Component Approach to Pyridine-Stabilized Ketenimines for the Synthesis of Diverse Heterocycles

“…34 1-(2-Amino-5-bromophenyl)ethan-1-one (4d) was prepared using known literature protocol. 35 1-(2-Amino-5-methoxyphenyl)ethan-1-one (4e) was prepared using known literature protocol. 36 3-Acetyl-4-aminobenzonitrile (4f) was prepared using known literature protocol.…”

Theoretical Investigations on the Rh(III)-Catalyzed Oxidative C–H Activation/Annulation of Salicylaldehydes with Masked Enynes: Mechanism Insights and Regioselectivity Origins

“…Chromones are a significant class of oxygen-containing heterocycles that are present in natural products and pharmaceuticals, exhibiting noteworthy biological activities such as anti-inflammatory, antimicrobial, antioxidant, and anticarcinogenic properties. , The synthesis of chromones can be accomplished through transition-metal-catalyzed sequential C–H activation/annulation of salicylaldehydes with suitable coupling partners. − Despite these advanced methods for constructing new skeleton molecules, there is still an urgent need to synthesize new related molecules, such as 3-vinyl chromone, which is found in many bioactive compounds and has antioxidant, antiproliferative, and PDE10 inhibitory activities, − and therefore remains of very important value in organic synthesis.…”