Within the framework of our attempts to synthesize pleiotropic anti-inflammatory agents, we have synthesized some chalcones and their corresponding 3,4-pyrrolyl derivatives. Chalcones constitute a class of compounds with high biological impact. They are known for a number of biological activities, including anti-inflammatory and free radical scavenging activities. They inhibit several enzymes i...

Herein we report the first example of the catalytic enantioselective addition of sodium bisulfite to a,b-unsaturated alkenes 1a–q which was achieved by the selection of an appropriate aminothiourea bifunctional catalyst (Scheme 1). Following the pioneering work carried out by the groups of Soo s, Connon, Deng, and Wang, bifunctional catalysis has matured to become a prominent area of organic sy...

Chalcones and their derivatives have been shown to have potent anticancer activity. However, the exact mechanisms of cytotoxic activity remain to be established. In this study, we have evaluated a series of boronic chalcones for their anticancer activity and mechanisms of action. Among the eight chalcone derivatives tested, 3,5-bis-(4-boronic acid-benzylidene)-1-methyl-piperidin-4-one (AM114) e...

Hepatocellular carcinoma (HCC) is one of the most commonly diagnosed cancers worldwide. Chemoprevention of HCC can be achieved through the use of natural or synthetic compounds that reverse, suppress or prevent the development of cancer progression. In this study, we investigated the antiproliferative effects and the mechanism of action of two compounds, 2,3,4'-trimethoxy-2'-hydroxy-chalcone (C...

Overactivation of the Wnt/β-catenin pathway in adult tissues has been implicated in many diseases, such as colorectal cancer. Finding chemical substances that can prevent this phenomenon is an emerging problem. Recently, several natural compounds have been described as Wnt/β-catenin inhibitors and might be promising agents for the control of carcinogenesis. Here, we describe two natural substan...

From an ethyl acetate-soluble fraction of the exudate obtained from the stems of Angelica keiskei (Umbelliferae), 17 compounds, viz. five chalcones (1-5), seven coumarins (6-12), three flavanones (13-15), one diacetylene (16), and one 5-alkylresorcinol (17), were isolated. These compounds were evaluated with respect to their inhibitory effects on the induction of Epstein-Barr virus early antige...

A series of hybrid of triazoloquinoxaline-chalcone derivatives 7a-k were designed, synthesized, fully characterized, and evaluated for their cytotoxic activity against three target cell lines: human breast adenocarcinoma (MCF-7), human colon carcinoma (HCT-116), and human hepatocellular carcinoma (HEPG-2). The preliminary results showed that some of these chalcones like 7b-c, and 7e-g exhibited...

Photoresponsive molecular devices can be a valuable tool to promote chemical changes in response multiple signals, such as photons and pH, deliver drugs or detect physiological conditions vivo. For example, trans-chalcones (Ct) from 4′-hydroxyflavylium (F1) 7-hydroxyflavylium (F2) undergo cis-trans isomerization by photoreaction into many different structures. The takes place at slow rate pH ch...

  Objective(s): Chalcones and their rigid analogues represent an important class of small molecules having anticancer activities. Therefore, in this study the synthesis and cytotoxic activity of new 3-benzylidenchroman-4-ones were described as rigid chalcone analogues.   Materials and Methods: The reaction of resorcinol with 3-chloropropionic acid in the presence of CF3SO3H was a...

Abstract: Aim/Background: Metastasis is the main reason of death in cancer with a key challenge to target it precisely by available treatments. The current study was designed assess anti-metastatic potentials synthesized chalcones, Ch-1 and Ch-2. Materials Methods: In vitro included cytotoxicity, scratch wound assay cell cycle analysis vivo performed C57BL/6 mice B16-F10 induced metastatic lung...