N-Heterocyclic functionalized chalcone derivatives as anti-inflammatory agents for atopic dermatitis treatment by inhibiting JAK1/STAT3 signaling pathway.

Atopic dermatitis (AD) is difficult to cure as a chronic inflammatory skin disease. In the present study, a series of N-heterocyclic functionalized chalcone derivatives have been prepared to investigate their in vitro and in vivo anti-inflammatory activities. The results indicated that many derivatives could effectively inhibit NO generation with low toxicity.

Benzofuran-Chalcone Derivatives as VEGFR-2 Inhibitors: Synthesis and Anticancer Evaluation.

The discovery and development of efficient VEGFR-2 inhibitors has become a research hotspot in cancer treatment. In this work, a series of new benzofuran-based chalcone derivatives have been prepared, and in vitro anticancer activities have been evaluated. The results revealed that derivatives showed selective cytotoxic activity against HCC1806, Hela, and A549 cell lines, especially 5c exhibited excellent inhibitory effect on VEFGR-2 (IC = 1.

Synthesis and antifungal evaluation of new azole derivatives containing 1,2,3-triazole.

Invasive fungal infections caused by are becoming increasingly serious and there is an urgent need for exploring new antifungal drugs. In the present work, a series of new azole derivatives containing a 1,2,3-triazole moiety have been prepared, and antifungal activity have been evaluated. The results revealed that most compounds showed excellent antifungal activity against SC5314 and drug-resistant SC5314-FR.

Synthesis and anti-tumor activity of new benzofuran-based chalcone derivatives as potent VEGFR-2 inhibitors.

Cancer is one of the most significant public health problems worldwide, and the discovery and development of efficient VEGFR-2 inhibitors has been a research hotspot in cancer treatment. In the present work, a series of novel benzofuran-based chalcone derivatives have been prepared, and anti-tumor activities of them have been evaluated. The results indicated that the compounds displayed potent anticancer activity against HCC1806, HeLa and A549 cell lines.

Development of new dehydrocostuslactone derivatives for treatment of atopic dermatitis inhibition of the NF-κB signaling pathway.

Atopic dermatitis (AD), a recurrent inflammatory systemic skin disease, is difficult to cure. In the present study, several ethylenediamine-derived dehydrocostuslactone (DHCL) derivatives were prepared to assess their and anti-inflammatory activities. The results indicated that DHCL derivatives inhibited NO generation with low cytotoxicity.

MW-19, a dihydropyrazole derivative, induces human triple-negative breast cancer cell apoptosis by targeting apoptosis-related pathways.

Previous studies have indicated that heterocyclic substituted dihydropyrazole derivatives, particularly MW-19, potentially exert anticancer activity in vitro; however, the underlying mechanism remains unknown. The present study was designed to investigate the mechanisms underlying MW-19 activity in triple-negative breast cancer cells. A sulforhodamine B assay was performed to evaluate cell proliferation inhibition rates, and the antitumor effect of MW-19 was evaluated in mice with HCC-1806 xenografts.

Discovery of novel chrysin derivatives as potential Anti-Psoriasis agents.

Psoriasis is a chronic inflammatory disease and is difficult to cure. In this work, a series of novel chrysin derivatives have been designed and prepared while evaluating anti-inflammatory activities in vitro and in vivo. In vitro, RAW264.

New azole derivatives linked to indole/indoline moieties combined with FLC against drug-resistant .

is the most common fungal pathogen associated with human opportunistic infections. Invasive infections caused by are becoming increasingly serious. However, with the rising incidence of fungal infection, many fungi are resistant to commonly used drugs.

Exploration of costunolide derivatives as potential anti-inflammatory agents for topical treatment of atopic dermatitis by inhibiting MAPK/NF-κB pathways.

Atopic dermatitis (AD) is a common inflammatory disease and it is very difficult to treat. In the present work, a series of costunolide derivatives have been prepared, and in vitro and in vivo anti-inflammatory activities have evaluated. The results showed that most derivatives displayed good inhibition of NO generation with low cytotoxicity, and 7d could inhibit the phosphorylation of P38, P65 NF-κB and IκB-α in LPS-induced RAW264.

Synthesis and Antifungal Evaluation of New Azole Derivatives against .

In this study, we designed and prepared a series of new azole derivatives by recombination of fluconazole (FLC) and ketoconazole units, and antifungal activities against were evaluated. The results indicated that most azoles showed good antifungal activity against the drug-sensitive strain, especially compounds , , , , , , , and , which displayed better antifungal activity (MIC < 1.0 μg/mL) than FLC against SC5314.

Optimization and antifungal activity of quinoline derivatives linked to chalcone moiety combined with FLC against Candida albicans.

In present work, a series of quinoline derivatives linked to chalcone moiety have been prepared, and their in vitro and in vivo antifungal activities against C. albicans have been evaluated. The results indicated that quinoline combined with fluconazole (FLC) showed good inhibitory activity against C.

Synthesis and Cytotoxic Activity of Quinazoline-benzofuran Conjugates.

Aims: In order to study on structure-activity relationships of benzofurans.

Background: Benzofuran is a kind of natural compound widely existing in nature with pharmacological effects. The development of new anticancer benzofuran derivatives has attracted more and more attention.

Anticancer evaluation of benzofuran derivatives linked to dipiperazine moiety.

In this work, a series of novel benzofuran derivatives linked to dipiperazine moiety have been prepared, and in vitro anticancer activity against Hela and A549 was investigated. The results demonstrated that benzofuran derivatives exerted potent antitumor effect. Especially, compounds 8c and 8d showed better antitumor activity against A549 (IC = 0.

Antifungal evaluation of quinoline-chalcone derivatives combined with FLC against drug-resistant Candida albicans.

With the widespread clinical use of FLC, the FLC-resistant C. albicans greatly increases the difficulty of treatment, and drug combination becomes an important method to treat C. albicans infection.

MW‑9, a chalcones derivative bearing heterocyclic moieties, attenuates experimental autoimmune encephalomyelitis via suppressing pathogenic T17 cells.

Previous studies have indicated that MW‑9, a chalcones derivative bearing heterocyclic moieties, has considerable anti‑inflammatory activity . Whether MW‑9 may be used to treat inflammation‑based diseases, such as multiple sclerosis, remains unknown. The present study was designed to determine the effect and underlying mechanism of MW‑9 in experimental autoimmune encephalomyelitis (EAE).

Discovery of novel indole and indoline derivatives against Candida albicans as potent antifungal agents.

With the widespread use of azole antifungals in the clinic, the drug resistance has been emerging continuously. In this work, we have designed and prepared a series of novel indole and indoline derivatives, and in vitro antifungal activity against C. albicans were evaluated.

Copper(II)-catalyzed Synthesis of Benzoxazoles from Inactive 2-chloroanilides.

Aim And Objective: Benzoxazoles are of great importance in natural products, pharmaceutical agents as well as synthetic intermediates. Although many works on the construction of benzoxazoles by Cu-catalyzed intramolecular O-arylation of ortho-haloanilides have been reported, only a few reports about transition metal-catalyzed synthesis of benzoxazoles from inactive 2-chloroanilides so far. This work aimed to explore a green and cheap protocol for intramolecular O-arylation of inactive 2-chloroanilides to prepare 2-arylbenzoxazoles.

Synthesis and antifungal evaluation of phenol-derived bis(indolyl)methanes combined with FLC against Candida albicans.

With the widespread use of azole antifungals in the clinic, the drug resistance has been emerging continuously. In this work, we focus on boron trifluoride etherate catalyzed condensation of indole and salicylaldehydes to form bis(indolyl)methanes (BIMs) in high yields, and in vitro antifungal activity against Candida albicans were evaluated. The results showed that most phenol-derived BIMs combined with fluconazole (FLC) exhibited good antifungal activity against sensitive and drug-resistant C.

Flower extract of . ameliorates DSS-induced ulcerative colitis by affecting TLR4/NF-B and TLR4/MAPK signaling pathway in a mouse model.

Objectives: This study aimed to find out the protective effects and preliminary mechanisms of the flower extract of (FEC) on dextran sulfate sodium salt (DSS)-induced colitis.

Materials And Methods: The ulcerative colitis models of mice induced by 3% DSS were established and treated with FEC. Body weight changes, disease activity index (DAI), colon histopathological score, anti-oxidant ability, and the level of inflammatory cytokines were determined.

Discovery of heterocyclic substituted dihydropyrazoles as potent anticancer agents.

In this work, a series of novel heterocyclic substituted dihydropyrazole derivatives have been prepared, and in vitro anticancer activity against a panel of human tumor cell lines by SRB were evaluated. The results indicated that piperazine substituted dihydropyrazole derivatives exhibited superior anticancer activity than that of other compounds. Especially, compounds 4g, 4h, 4l, 4m, 4o, 6g, 6j and 6l showed potent antitumor activity.

Cu(II)/Vasicine Promoted Intramolecular C-O Formation: Synthesis of Benzoxazoles in EtOH.

Aims And Objectives: Benzoxazoles are valuable bicyclic aromatic compounds; the construction of benzoxazoles via C-O cross-coupling reactions has attracted more and more attention.

Materials And Methods: The best condition of C-O bond formation from o-haloanilides was carried out, taking Cu(OTf) (5 mol%) and vasicine (10 mol%) as the catalysts in EtOH in the presence of KCO (2 eq.) for 12 h at 90°C.

Synthesis of New Piperazine Substituted Chalcone Sulphonamides as Antibacterial Agents.

Background: Infection is a global threat to human health, and there is an urgent need to develop new effective antibacterial drugs to treat bacterial infections.

Objective: To study the antibacterial activity of piperazine substituted chalcone sulphonamides.

Materials And Methods: A series of novel piperazine substituted chalcone sulphonamides have been prepared, and in vitro antibacterial activity against Staphylococcus aureus, Bacillus subtilis and Escherichia coli strains were evaluated.

Efficient Cu-catalyzed intramolecular -arylation for synthesis of benzoxazoles in water.

An efficient method was developed for synthesis of benzoxazoles by Cu-catalyzed intramolecular -arylation of -halobenzanilides in water. This strategy provides several advantages, such as high yields, water as a green solvent and functional groups tolerance.

Synthesis and anti-inflammatory evaluation of new chalcone derivatives bearing bispiperazine linker as IL-1β inhibitors.

In this work, a series of novel chalcone derivatives bearing bispiperazine linker have been synthesized and in vitro anti-inflammatory, cytotoxic activity and anti-inflammatory mechanism have been screened. The results indicated that most bispiperazinochalcone derivatives displayed good inhibition of NO (IC < 20 μM) and low cytotoxicity (CC > 40 μM), and selectively inhibited the production of IL-1β via inhibiting NLRP3 inflammasome activation, as promising candidate compounds for the treatment of NLRP3 inflammasome-driven diseases.

A Brief Synthesis of 2,2'-Arylmethylene Bis(3-hydroxy-5,5-dimethyl-2-cyclohexene-1- one) Catalyzed by TEAOH in Various Solvents.

Aims And Objectives: 2,2'-Arylmethylene bis(3-hydroxy-5,5-dimethyl-2-cyclohexene-1-one) having four carbonyl functionalities along with their tautomeric keto-enol forms, is an important biologically active compound and important synthetic intermediate in the synthesis of xanthenes. This study was conducted in order to develop a new and concise method of synthesis of 2,2'-arylmethylene bis (3-hydroxy-5,5-dimethyl-2- cyclohexene-1-one) derivatives.

Materials And Methods: TEAOH (20 mol %) was fond to be as a simple and efficient catalyst for the preparation of 2,2'-arylmethylene bis(3-hydroxy-5,5-dimethyl-2-cyclohexene-1-one) derivatives by the Knoevenagel condensation/Michael addition tandem reactions.