Palladium-Catalyzed Four-Component Radical Cascade Carbonylation Access to 2,3-Disubstituted Benzofuran Derivatives.

Multicomponent radical tandem reactions have emerged as a crucial technique for synthesizing complex molecules in organic chemistry. In this study, we report a palladium-catalyzed four-component difluoroalkylative carbonylation of enynes and ethyl difluoroiodoacetate. This transformation proceeds through a multistep sequential reaction that introduces reactive difluoro and carbonyl groups while constructing the benzofuran skeleton.

Nickel-Catalyzed Narasaka-Heck Cyclization Carbonylation of Unsaturated Oxime Esters with Arylboronic Acids.

The Narasaka-Heck reaction is one of the most straightforward methods for constructing pyrroline derivatives. Herein, we report a novel nickel-catalyzed three-component carbonylation reaction, which cleverly realizes the continuous construction of C(sp)-N bonds and C(sp)-C(sp) bonds and effectively promotes the synthesis of acyl-substituted pyrroline derivatives. Furthermore, this strategy not only expands the conversion pathway of γ,δ-unsaturated oxime esters but also provides a new method for the synthesis of nitrogen-containing heterocyclic compounds.

Redox Neutral Radical-Relay Nickel-Catalyzed Remote Carbonylation.

A novel and efficient method for the catalytic installation of a carbonyl group via remote radical coupling is disclosed. The nickel-catalyzed reaction proceeds to undergo a sequential single-electron transfer, 1,5-hydrogen atom transfer, and carbonyl insertion, thus providing the α-substituted ketone. Further, this reaction could be carried out smoothly under normal pressure and redox-neutral conditions, and demonstrated functional-group compatibility and excellent site-selectivity.

Design, Synthesis and Cytotoxicity Evaluation of Novel Indole Derivatives of Panaxadiol.

Based on the well-known cytotoxicity of indole compounds, we used the 'Fisher indole synthesis' method to introduce appropriately substituted indole rings into panaxadiol (PD), generating eighteen novel Panaxadiol indole derivatives. Six human cancer cell lines (A549, HepG-2, HCT-116, SGC-7901, MDA-MB-231, PC-3 cells) and one normal ovarian cell lines (IOSE144) were designed to evaluate the anti-proliferative activity of the PD derivatives. The results showed that the majority of PD derivatives showed enhanced anti-proliferative activity, when compared with PD, with P-Methylindolo-PD exhibiting the highest cytotoxicity.

Synthesis and biological evaluation of heterocyclic ring-fused dammarane-type ginsenoside derivatives as potential anti-tumor agents.

Twenty-one AD-1 derivatives were designed and synthesized by introducing various nitrogen-containing heterocycles into C-2 and C-3 positions. Their anti-proliferative activities were evaluated on two human cancer cell lines (HCT-116 and RM-1 cells) and one normal human gastric mucosal epithelial cell GES-1. Most of derivatives exhibited increased inhibitory potency, compared with lead compound AD-1.

Cedrol from Ginger Ameliorates Rheumatoid Arthritis via Reducing Inflammation and Selectively Inhibiting JAK3 Phosphorylation.

Ginger, as a food spice, is widely applied due to its extensive effects. Cedrol (CE) found in ginger is a sesquiterpene with anti-inflammatory activity. The objective of this research is to discuss the efficacy of CE on ameliorating rheumatoid arthritis (RA).

Novel ginsenoside derivatives have shown their effects on PC-3 cells by inducing G1-phase arrest and reactive oxygen species-mediate cell apoptosis.

In this study, piperazine groups were introduced into ginsenoside to enhance its ability to induce Reactive Oxygen Species (ROS) production and apoptosis in cancer cells. In total, 27 ginsenoside piperazine derivatives were synthesized and tested for their anti-proliferative activity in cancer cell lines by MTT assay. The results showed that compounds 4a, 4g, 4f, 4i, 5g, 5i, 6a, 6g, 6f and 6i had significant inhibitory effects on cancer cell growth.

Hypoglycemic Effects of Licochalcone A on the Streptozotocin-Induced Diabetic Mice and Its Mechanism Study.

Type 2 diabetes mellitus (T2DM) is a type of metabolic illness based on relatively insufficient insulin secretion and insulin resistance (IR) as pathophysiological bases. Currently, it is the main type of diabetes. Hypoglycemic and hypolipidemic effects of licochalcone A (LicA) on high-fat diet and streptozocin-caused T2DM were studied.

Synthesis and anti-cancer activity studies of dammarane-type triterpenoid derivatives.

Two series of novel derivatives of AD-2, an active ginsenoside derived from ginseng were designed and synthesized. Five human cancer cell lines (MGC-803, SGC-7901, A549, MCF-7, PC-3 cells) and one normal ovarian cell IOSE144 were employed to evaluate the anti-proliferative activity. Most of derivatives possessed obvious enhanced activity compared with AD-2.

A Noncontact Breathing Disorder Recognition System Using 2.4-GHz Digital-IF Doppler Radar.

In this paper, a noncontact breathing disorder recognition system has been proposed for identifying irregular breathing patterns. The proposed system consists of a Doppler radar-based sensor module and a machine-learning-based breathing disorder recognition module. A custom-designed 2.