INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2021
·Vol. 22
·期 16
·8949
·
IF 5.924
Huiqing Luo,Na Li,Liyan Liu,Huaqiao Wang,Feng He
Fluorophores with aggregation-induced emission enhancement (AIEE) properties have attracted increasing interest in recent years. On the basis of our previous research, we successfully designed and synthesized eleven chalcones. Through an optical performance experiment, we confirmed that compounds1–6had obvious AIEE properties. As these AIEE molecules had excellent fluorescence properties and a large Stokes shift, we studied their application in living cell imaging, and the results showed that these compounds had low cytotoxicity and good biocompatibility at the experimental concentrations. More importantly, they could specifically label mitochondria. Subsequently, we selected zebrafish as experimental animals to explore the possibilities of these compounds in animal imaging. The fluorescence imaging of zebrafish showed that these AIEE molecules can enter the embryo and can be targeted to aggregate in the digestive tract, which provides a strong foundation for their practical application in the field of biological imaging. Compared with traditional fluorophores, these AIEE molecules have the advantages of possessing a small molecular weight and high flexibility. Therefore, they have excellent application prospects in the field of biological imaging. In addition, the findings of this study have very positive practical significance for the discovery of more AIEE molecules.Keywords:AIEE;chalcone;mitochondria;zebrafish
研究领域:
生物成像
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分子生物学
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材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
SYNTHESIS-STUTTGART
·
2015
·Vol. 48
·期 02
·231-237
·
IF 2.689
Yongbo Zhou,Zhongwen Li,Xiao Yang,Xiulin Chen,Mei Li,Tieqiao Chen,Shuang-Feng Yin
A simple and environmentally benign method was developed for the synthesis of chalcones in high to excellent yields by a phosphorous acid promoted alkyne–aldehyde hydration–condensation in an oil/water two-phase system. The method is the first efficient protocol for the preparation of chalcones that is mediated by a simple Brønsted acid in a two-phase system.
研究领域:
有机化学
·
绿色化学
✓ 已验证
DOI
高影响因子
JOURNAL OF CHEMICAL RESEARCH
·
2023
·
IF 1.4
Bin Gao,Yanhua Wang
The selective hydrogenation of chalcone to dihydrochalcone under atmospheric hydrogen pressure is investigated using a thermoregulated phase-transfer ruthenium nanocatalyst, representing the first ruthenium nanocatalyst used for this reaction. Under the optimal conditions, the conversion of chalcone into dihydrochalcone and the selectivity are 98% and >99%, respectively. The ruthenium catalyst can be easily separated from the product and recycled three times without any decrease in the conversion or selectivity. The turnover frequency is higher than that of a reported ruthenium complex catalyst. The thermoregulated phase-transfer ruthenium nanocatalyst is also applied for the atmospheric hydrogenation of other α,β-unsaturated ketones.
研究领域:
催化
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有机化学
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纳米技术
✓ 已验证
产品关联
DOI
高影响因子
TETRAHEDRON
·
2023
·
IF 2.1
Zifan Zhu,Xiaoqing Feng,Hecheng Wang,Jiaru Fan,Chen Zhang,Guoqiang Song,Long Tang
Coumarin and chalcone are two compounds that have been extensively studied for their neuroprotective effects. Coumarin is known for its ability to inhibit MAO activity in the brain and reduce central nervous system damage caused by dopamine degradation. Chalcone, on the other hand, has gained attention due to its potential medicinal value, including free radical scavenging, anti-inflammatory, and neuroprotective properties. Both compounds have shown promise in the development of treatments for neurodegenerative diseases like Alzheimer's disease . In this study, we designed and synthesized 36 coumarin-chalcone heteroderivatives based on the principle of structure hybridization . We then evaluated the inhibitory effects of these compounds on phosphodiesterase II (PDE2) at the enzyme level and analyzed their structure-activity relationship. Among the hybrid derivatives, compounds 2b , 3a , 3i , 3m , and 1l demonstrated significant inhibitory activity on PDE2, with IC50 values of 24.46 μM , 16.82 μM , 28.13 μM , 21.88 μM , and 29.72 μM , respectively. This paper presents the design, synthesis, and biological evaluation of coumarin-chalcone hybrid derivatives for their potential as PDE2 inhibitors.
研究领域:
药物化学
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神经科学
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2023
·Vol. 24
·期 21
·15549
·
IF 5.6
Weihong Lai,Jiaxin Chen,Xinjiao Gao,Xiaobao Jin,Gong Chen,Lianbao Ye
Chalcone is a common simple fragment of natural products with anticancer activity. In a previous study, the research group discovered a series of chalcone derivatives with stronger anticancer activities. To find better anticancer drugs, novel chalcone derivativesA1–A14,B1–B14have continuously been designed and synthesized. The antiproliferative activity of these compounds against breast cancer cells (MCF-7) was investigated by the Cell Counting Kit-8 (CCK-8) method with 5-fluorouracil (5-Fu) as the control drug. The results showed that compoundA14exhibited excellent antiproliferative ability compared to the control drug 5-Fu. Scratch experiments and cloning experiments further confirmed that compoundA14could inhibit the proliferation and colony formation activity of MCF-7 cells. In addition, molecular docking primarily explains the interaction between compound and protein. These results suggested that compoundA14could be a promising chalcone derivative for further anti-breast cancer research.Keywords:chalcones;synthesis;anti-breast cancer (MCF-7);molecular docking
研究领域:
药理学
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肿瘤学
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药物化学
✓ 已验证
DOI
PubMed
高影响因子
SYNTHETIC COMMUNICATIONS
·
2021
·
IF 2.007
Xiaoyun Ma,Daoping Wang,Gang Wei,Qingdi Zhou,Xiuhai Gan
Two series of quinoxaline–chalcone conjugates have been prepared by aldolic condensation and aromatic nucleophilic substitution reaction, and their anticancer activity against three cancer cell lines including benign prostatic hyperplasia epithelial cell (BPH-1), neuron-like rat pheochromocytoma cell line (PC12) and human breast cancer cell line (MCF-7) were evaluated in vitro. All of the synthesized compounds exhibited moderate to good activity against the cancer cell lines selected. Particularly, Compound A5 showed the excellent potent activity against BPH-1 and MCF-7 with IC50 values of 10.4 and 9.1 μM, respectively, which is similar to doxorubicin (14.1 and 9.2 μM, respectively). As well as compound B6 exhibited most excellent activity toward PC12 with IC50 values of 16.4 μM. Compound A10 exhibited 55.4, 36.8 and 54.5 folds higher selectivity for BPH-1, PC12 and MCF-7 cells than for HEK-293 cell, respectively. In addition, theoretical biological activities of compounds A5 and A10 were evaluated by SwissADME.
研究领域:
药物化学
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肿瘤学
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有机合成
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY A-CHEMISTRY
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2022
·
IF 5.141
Hongxiang Li,Chunyue Zhao,Zhen Wang,Jinfeng Xing
The application of drug-loaded nanogels in the treatment of cancer has attracted much attention. Here, the stability of chrysin under green LED was investigated, the nanogels loaded with chrysin in situ were prepared and the effect of chrysin in the polymerization reaction was investigated. The morphology, chemical structure, and drug-polymer interactions of the nanogels loaded with chrysin (NG-C) were studied. Moreover, the time of gel point appearance and double bond conversion were also evaluated.
研究领域:
药学
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材料科学
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肿瘤学
✓ 已验证
产品关联
DOI
高影响因子
CRYSTAL GROWTH & DESIGN
·
2022
·
IF 4.01
Kai Xu,Rui Chen,Jinkang Ma,Tianhua Wang,Degao Zhong,Lifeng Cao,Bing Teng,Haitao Wu
Chalcone structures obtained by structural tailoring are an important class of molecular organic nonlinear optics (NLO) crystals that can be used for multiple purposes. In this work, two novel chalcone compound crystals with non-centrosymmetric structures, 6MN3MPP (C21H18O3, Pca21) and 6MN4MPP (C21H18O3, Pn), were designed and grown by extending the π-conjugation and structure-modifying strategy. On this basis, the second harmonic generation (SHG) efficiency, thermal stability, transmission spectra, dielectric constant, and photoluminescence properties of the crystal were characterized, and the hyperpolarizability of the crystal was theoretically calculated. The results show that the synthesized crystals exhibit higher crystal transparency (≥70%), higher melting point, and lower dielectric constant (εr ≈ 6.5) compared with other reported chalcone NLO crystals. In particular, the SHG intensity of the 6MN3MPP crystal is 4.3 times higher than that of the KDP crystal. All of the results show that the two newly synthesized compounds have good application prospects as NLO crystals.
研究领域:
材料科学
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晶体学
·
分子设计
✓ 已验证
DOI
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2025
·
IF 4.7
Yaqi Qin,Xueting Mu,Xiaoyu Feng,Kai Xu,Jinkang Ma,Lifeng Cao,Bing Teng
Two novel chalcone crystals, FTB (C 13 H 9 BrO 2 , P 2 1 ) and FTC (C 13 H 9 ClO 2 , Pna 2 1 ), were successfully synthesized by introducing halogen substituents, and slow evaporation method was used for these two crystals growth. The molecular stacking and arrangement of these two crystals were analyzed by using single-crystal XRD technique. The SHG intensities of the FTB and FTC crystals were 14.4 and 12.6 times higher than the simultaneously measured KDP. Their cutoff wavelengths are 350 nm and 346 nm, respectively. FTC crystals show higher thermal decomposition temperature (T m ≈ 146 °C) and FTB crystals show higher optical energy gap (E g = 3.63 eV) than other reported chalcone crystals. All the results show that these two newly grown crystals are optically promising.
研究领域:
材料科学
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化学
✓ 已验证
产品关联
DOI
高影响因子
BRAZILIAN JOURNAL OF MEDICAL AND BIOLOGICAL RESEARCH
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2023
·
IF 2.3
Omidi-Shahsavandi M.,Yaghmaei P.,Ahmadian S.,Ebrahim-Habibi A.
Amyloid fibrils are characteristic of several disorders including Alzheimer's disease (AD), with no cure or preventive therapy. Diminishing amyloid deposits using aromatic compounds is an interesting approach toward AD treatment. The present study examined the anti-fibrillogenic effects of silibinin and trans-chalcone in vitro, in vivo, and in silico on insulin amyloids. In vitro incubation of insulin at 37°C for 24 h induced amyloid formation. Addition of trans-chalcone and silibinin to insulin led to reduced amounts of fibrils as shown by thioflavin S fluorescence and Congo red absorption spectroscopy, with a better effect observed for silibinin. In vivo bilateral injection of fibrils formed by incubation of insulin in the presence or absence of silibinin and trans-chalcone or insulin fibrils plus the compounds in rats' hippocampus was performed to obtain AD characteristics. Passive avoidance (PA) test showed that treatment with both compounds efficiently increased latency compared with the model group. Histological investigation of the hippocampus in the cornu ammonis (CA1) and dentate gyrus (DG) regions of the rat's brain stained with hematoxylin-eosin and thioflavin S showed an inhibitory effect on amyloid aggregation and markedly reduced amyloid plaques. In silico, a docking experiment on native and fibrillar forms of insulin provided an insight onto the possible binding site of the compounds. In conclusion, these small aromatic compounds are suggested to have a protective effect on AD.
研究领域:
神经科学
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药理学
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分子生物学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF FLUORESCENCE
·
2023
·Vol. 34
·期 4
·1603-1615
·
IF 2.7
Yang Yun-Shang,Yuan Yi-Zhen,Zhang Ying-Peng,Guo Hui-Chen,Xue Ji-Jun
Widely utilized in the chemical industry and agriculture, hydrazine is easily absorbed by living things and can cause physical harm when in touch for an extended period of time. As a result, a novel cinnamaldehyde chalcone C5 was produced by Friedel Crafts process and aldol condensation reaction. Triphenylamine was used as the raw material for hydrazine determination in both reactions. Chalcone C5 exhibits significant AIE behavior in a mixed mixture of ethanol and water in addition to having great selectivity and a low detection limit (0.119 nm) for hydrazine. The solvent effect test revealed a linear relationship between the Stokes shift of C5 in the solvent and the rise in solvent orientation polarization. It is important to note that C5 is not harmful to MCF-7 cells, mouse kidney cells, or pig kidney cells. Furthermore, research on cell imaging has demonstrated that probe C5 may be utilized to image the fluorescence of hydrazine in active MCF-7 cells.
研究领域:
化学
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生物医学
·
材料科学
✓ 已验证
DOI
高影响因子
KEY ENGINEERING MATERIALS
·
2019
·
IF 0
Yan Kai Huang,Qi Lin Mei,Zhi Xiong Huang,Yan Qin,Di Zhu
In this paper, the structure of the photosensitive diamines was designed and the method of synthesizing such diamines was investigated. The 1-(3-aminophenyl)-3-(4-aminophenyl)-2-propen-1-one analyzed by elemental analysis and infrared analysis was synthesized through two-step experiments with Aldol condensation and Nitroammoniation process. Through the experiment the optimum reaction conditions are raw material ratio of 1:1, anhydrous ethanol dosage of 60 ml, 10 % NaOH dosage of 10 ml and reaction temperature of 25°C for 4h. The yield was about 55.4 %.
研究领域:
有机化学
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材料科学
✓ 已验证
产品关联
DOI
危险品化学品经营许可证（带存储）