Discovery of 4-((E)-3,5-dimethoxy-2-((E)-2-nitrovinyl)styryl)aniline derivatives as potent and orally active NLRP3 inflammasome inhibitors for colitis.

NLRP3 inflammasome activation plays a key role in a variety of inflammatory diseases as IBD. Here a series of pterostilbene derivatives were designed and synthesized based on previous SAR, leading to discovery of new effective NLRP3 inflammasome inhibitors with metabolic stability. Among them, the most effective compound 27 showed high inhibitory efficacy (against IL-1 β: IC = 1.

Discovery of Novel Pterostilbene-Based Derivatives as Potent and Orally Active NLRP3 Inflammasome Inhibitors with Inflammatory Activity for Colitis.

Studies have shown that the abnormal activation of the NLRP3 inflammasome is involved in a variety of inflammatory-based diseases. In this study, a high content screening model targeting the activation of inflammasome was first established and pterostilbene was discovered as the active scaffold. Based on this finding, total of 50 pterostilbene derivatives were then designed and synthesized.

Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.

In order to discover and develop drug-like anti-inflammatory agents against arthritis, based on "Hit" we found earlier and to overcome drawbacks of toxicity, twelve series of total 89 novel pyrimidine, pyrazolo[4,3-d]pyrimidine and thieno[3,2-d]pyrimidine derivatives were designed, synthesized and screened for their anti-inflammatory activity against NO and toxicity for normal liver cells (LO2). Relationships of balance toxicity and activity have been summarized through multi-steps, and title compounds 22o, 22l were found to show lower toxicity (against LO2: IC = 2934, 2301 μM, respectively) and potent effect against NO release (IR = 98.3, 97.

Novel phthalide derivatives: Synthesis and anti-inflammatory activity in vitro and in vivo.

Phthalide is a promising chemical scaffold and has been proved to show potent anti-inflammatory efficacy. In this study, three series, total of 31 novel phthalide derivatives were designed and synthesized, their anti-inflammatory activities were screened in vitro and in vivo. The anti-inflammatory activity of all the compounds were screened on LPS induced NO production to evaluating their inhibitory effects.

Synthesis and biological evaluation of myricetin-pentadienone hybrids as potential anti-inflammatory agents in vitro and in vivo.

Some important pro-inflammatory cytokines such as interleukin-6, tumor necrosis factor-α and nitric oxide are thought to play key roles in the destruction of cartilage and bone tissue in joints affected by rheumatoid arthritis. In the present study, a series of new myricetin-pentadienone hybrids were designed and synthesized. Majority of them effectively inhibited the expressions liposaccharide-induced secretion of IL-6, TNF-α and NO in RAW264.

Catalytic hydrothermal liquefaction of rice straw for production of monomers phenol over metal supported mesoporous catalyst.

The catalytic (SBA-15, Ni/SBA-15, Al/SBA-15 and Ni-Al/SBA-15) hydrothermal liquefaction (HTL) of rice straw biomass was examined at different temperature with different amount of catalyst in the presence of different solvents. In comparison with water solvent liquefaction, the bio-oil yield significantly increased under alcoholic solvent (ethanol and methanol). The highest bio-oil yield was observed for water (44.

Synthesis and and anti-inflammatory activity of novel 4-ferrocenylchroman-2-one derivatives.

A series of novel 4-ferrocenylchroman-2-one derivatives were designed and synthesised to discover potent anti-inflammatory agents for treatment of arthritis. All the target compounds had been screened for their anti-inflammatory activity by evaluating the inhibition effect of LPS-induced NO production in RAW 264.7 macrophages.

Design and synthesis of novel pyrazolo[4,3-]pyrimidines as potential therapeutic agents for acute lung injury.

Four series of total 35 new pyrazolo[4,3-]pyrimidine compounds were designed, synthesized and evaluated for their inhibitory activity against LPS-induced NO production in RAW264.7 macrophages. Among them, compound was found to be the most potent inhibitor, which decreased the production of cytokines , such as NO, IL-6 and TNF-α, with IC values of 2.

Novel resveratrol-based flavonol derivatives: Synthesis and anti-inflammatory activity in vitro and in vivo.

In order to discover novel anti-inflammatory agents, total thirty-seven new resveratrol-based flavonol derivatives were designed and synthesized. All compounds have been screened for their anti-inflammatory activity by evaluating their inhibition effect of LPS-induced NO production in RAW 264.7 macrophages.

Novel Pyrazolo[4,3- d]pyrimidine as Potent and Orally Active Inducible Nitric Oxide Synthase (iNOS) Dimerization Inhibitor with Efficacy in Rheumatoid Arthritis Mouse Model.

In order to discover novel anti-inflammatory agents for treatment of arthritis and based on preliminary structure-activity relationships, four series (A-D) of total 90 new pyrazolo[4,3- d]pyrimidine compounds were designed and synthesized. All the compounds have been tested for their anti-inflammatory activities by inhibiting of LPS-induced NO production. A clear structure-activity relationship has been concluded step by step, and finally 3,4,5-trimethoxystyryl-1 H-pyrazolo[4,3- d]pyrimidine was found to be the most active scaffold.

Discovery of new chromen-4-one derivatives as telomerase inhibitors through regulating expression of dyskerin.

A series of new trimethoxyphenyl-4H-chromen derivatives as telomerase inhibitors through regulation dyskerin were designed and synthesised. The anticancer activity assay in vitro showed that compound 5i 3-(4-(4-isonicotinoylpiperazin-1-yl)butoxy)-5,7-dimethoxy-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one exhibited high activity against Hela, SMMC-7721, SGC-7901, U87 and HepG2 cell lines. Compound 5i also showed potent inhibitory activity against telomerase.

New pentadienone oxime ester derivatives: synthesis and anti-inflammatory activity.

To develop novel anti-inflammatory agents, a series of new pentadienone oxime ester compounds were designed and synthesized. The structures were determined by IR, H NMR, C NMR, and HRMS. All compounds have been screened for their anti-inflammatory activity by evaluating their inhibition against LPS-induced nitric oxide (NO) release in RAW 264.

Discovery of (4-bromophenyl)(3-hydroxy-4-methoxyphenyl)methanone through upregulating hTERT induces cell apoptosis and ERS.

Dominant-negative mutants of telomerase hTERT were demonstrated to have selective effects in tumor cells. However, no any effective and highly selective hTERT inhibitor has been developed so far. We focused on developing new hTERT modulators and synthesized a small molecular compound, named (4-bromophenyl)(3-hydroxy-4-methoxyphenyl)methanone.

New arylpyrazoline-coumarins: Synthesis and anti-inflammatory activity.

To develop new anti-inflammatory agents with improved pharmaceutical profiles, a series of new phenyl-pyrazoline-coumarin derivatives (4a∼4m) were designed and synthesized. Compounds 4a and 4b were determined by X-ray crystallography. All of the compounds have been screened for their anti-inflammatory activity characterized by evaluating their inhibition against LPS-induced IL-6 release.

Diarylpentadienone derivatives (curcumin analogues): Synthesis and anti-inflammatory activity.

A series of new (2E,4E)-1-(substitutedphenyl)-5-(substitutedphenyl)penta-2,4-dien-1-one derivatives were designed and synthesized. Compounds 3i, 3k were determined by X-ray. All of the compounds have been screened for their anti-inflammatory activity characterized by evaluating their inhibition against LPS-induced IL-6 and TNF-α release in cell RAW 264.

Benzophenone-nucleoside derivatives as telomerase inhibitors: Design, synthesis and anticancer evaluation in vitro and in vivo.

Based on telomerase, thirteen novel phenstatin moiety linked stavudine derivatives (8a∼8e and 11a∼11f) were synthesized. The structures were determined by NMR and TOF-HRMS. The screening results showed that some compounds had better anti-cancer activity in vivo and in vitro.

A highly selective chemosensor for Al3+ based on 2-oxo-quinoline-3-carbaldehyde Schiff-base.

A new Schiff-base ligand (1) with good fluorescence response to Al(3+), derived from 2-oxo-quinoline-3-carbaldehyde and nicotinic hydrazide, had been synthesized and investigated in this paper. Spectroscopic investigation revealed that the compound 1 exhibited a high selectivity and sensitivity toward Al(III) ions over other commonly coexisting metal ions in ethanol, and the detection limit of Al(3+) ions is at the parts per billion level. The mass spectra and Job's plot confirmed the 1:1 stoichiometry between 1 and Al(3+).

A highly selective turn-on fluorescent chemosensor for zinc ion in aqueous media.

In the paper, a novel rhodamine6G based fluorescent chemosensor bearing 3-carbaldehyde chromone was designed and synthesized. According to the fluorescence behavior toward several metal ions, it showed highly selectivity and sensitivity to Zn(II) over other commonly coexistent metal ions (Cu(II), Cd(II), Hg(II), Mg(II), K(I), Pb(II), Fe(III) and Cr(III)) in aqueous environment (pH = 7.4).

An effective Cu(II) quenching fluorescence sensor in aqueous solution and 1D chain coordination polymer framework.

In the article, a novel fluorescent probe for the copper cation based on fluorescence quenching mechanism was designed. It exhibited high selectivity for Cu(II) over other common metal ions in aqueous media. Furthermore the coordination between Cu(II) and the organic molecule sensor fabricated an interesting 1D chain coordination polymer framework.

Synthesis, characterization, DNA binding properties and antioxidant activity of Ln(III) complexes with Schiff base ligand derived from 3-carbaldehyde chromone and aminophenazone.

A novel Schiff base ligand, chromone-3-carbaldehyde-aminophenazone (L) and its Ln(III) (Ln = La, Yb) complexes were synthesized and characterized by physicochemical methods. The interaction between the ligand, Ln(III) complexes and calf thymus DNA in physiological buffer (pH=7.10) was investigated by using UV-vis spectroscopy, fluorescence spectra, ethidium bromide experiments and viscosity measurements, indicating that the studied compounds can all bind to DNA via an intercalation binding mode and the complexes have stronger binding affinity than the free ligand alone.

Crystal structures, DNA-binding and cytotoxic activities studies of Cu(II) complexes with 2-oxo-quinoline-3-carbaldehyde Schiff-bases.

Three novel 2-oxo-quinoline-3-carbaldehyde Schiff-bases and their Cu(II) complexes were synthesized. The molecular structures of Cu(II) complexes were determined by X-ray crystal diffraction. The DNA-binding modes of the complexes were also investigated by UV-vis absorption spectrum, fluorescence spectrum, viscosity measurement and EB-DNA displacement experiment.

Synthesis, crystal structure, DNA interaction and antioxidant activities of two novel water-soluble Cu2+ complexes derivated from 2-oxo-quinoline-3-carbaldehyde Schiff-bases.

Two novel 2-oxo-quinoline-3-carbaldehyde (4'-hydroxybenzoyl) hydrazone, thiosemicarbazone ligands and its corresponding Cu(2+) complexes were synthesized, and the two complexes' structures were determined by X-ray single crystal diffraction. The interaction of the two Cu(2+) complexes with calf thymus DNA (CT-DNA) was investigated by electronic absorption spectroscopy, fluorescence spectroscopy and viscosity measurement. The experimental evidences indicated that the two water-soluble Cu(2+) complexes could strongly bind to CT-DNA via an intercalation mechanism.