EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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2020
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IF 5.573
Heping Zhu,Shilong Ying,Bingluo Zhou,Xiao Liang,Quan He,Ping Song,Xinyang Hu,Keqiang Shi,Mingteng Xiong,Hongchuan Jin,Yuanjiang Pan
Microtubules play a vital role in cell mitosis. Drugs targeting taxol or vinca binding site of tubulin have been proved an effective way to against cancer. However, drug resistance and cancer recurrence are inevitable, there is an urgent need to search for new microtubule-targeting agents (MTAs). In our study, a series of novel 2-aryl-3-sulfonamido-pyridines ( HoAns ) had been designed, synthesized, and evaluated for their antiproliferative activities in vitro and in vivo . Among them, compound HoAn32 exhibited the most potent activity with IC 50 values ranging from 0.170 to 1.193 μ M in a panel of cancer cell lines. Mechanism studies indicated that compound HoAn32 bound to the colchicine site of β-tubulin, resulting in colony formation inhibition, G2/M phase cell cycle arrest, cell apoptosis as well as increased the generation of ROS in both RKO and SW620 cells. In addition, compound HoAn32 showed potent anti-vascular activity in vitro . Furthermore, compound HoAn32 also exhibited outstanding antitumor activity in SW620 xenograft tumor models without observable toxic effects, which was more potent than that of ABT-751 . In conclusion, our findings suggest that compound HoAn32 may be a promising microtubule destabilizing agent and deserves for further development in cancer therapy.
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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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2014
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IF 3.432
Wenlin Xie,Shimin Xie,Ying Zhou,Xufu Tang,Jian Liu,Wenqian Yang,Minghua Qiu
A series of 5,6-disubstituted pyridine-2,3-dione-3-thiosemicarbazone derivatives(2a-2n) and 5,6-disubstituted pyridine-2,3-dione S-benzyl-3-thiosemicarbazones(3a-3g) were synthesized starting from 2,3-dihydroxypyridine via oxidation-Michael additions, condensations and nucleophilic substitutions. The structures of the compounds were established by IR, 1 H NMR, 13 C NMR, and HRMS . All newly synthesized compounds were screened for their anticancer activity against Breast cancer (MCF-7), Colon cancer (HCT-116) and hepatocellular cancer (BEL7402) cell lines. Bioassay results indicated that most of the prepared compounds exhibited cytotoxicity against various cancer cells in vitro. Some of the compounds exhibited promising antiproliferative activity , which were comparable to the positive control (5-fluorouracil). The structure–activity relationship was discussed.
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Catalysis Science & Technology
·
2023
·Vol. 13
·期 24
·7046-7058
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IF 5
Wei Jin,Dekang Liu,Liyuan Zhang,Qian Sun,Yishan Wang,Enzhou Liu,Xiaoyun Hu,Hui Miao
Titanium dioxide (TiO2), a conventional n-type semiconductor, was widely used in photocatalysis, electrocatalysis and photoelectrocatalysis due to its good UV absorption and stable physical and chemical properties. However, its wide band gap and low oxygen reaction (OER) activity limited its application in photoelectrochemical (PEC) water splitting. In this work, we successfully constructed type-II Sb2(S,Se)3@TiO2 core–shell heterojunctions. Antimony sulfide selenide (Sb2(S,Se)3) was a quasi-one-dimensional light-absorbing material with an adjustable band gap (1.1–1.8 eV), which broadened the TiO2 light absorption range and effectively promoted the photogenerated carrier separation, transportation and utilization. Of particular note, novel Sb2(S,Se)3 nanospheres (NSPs) (ca. 69 nm) were in situ grown inside the tubes attributed to the unique space-confinement effect of TiO2 nanotubes (NTs). The IPCE value for Sb2(S,Se)3@TiO2 at 734 nm was 10.808% compared to 0.030% for TiO2. The separation efficiency and injection efficiency increased from 2.48% and 31.62% to 4.90% and 36.48%, respectively. The onset potential was moved negatively by 60 mV, and the maximum photocurrent density of 1.53 mA cm−2 at 1.23 V vs. RHE was 13.9 times higher than that of TiO2 (0.11 mA cm−2). This work provided a new idea for the application of TiO2 in the field of PEC water splitting.
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CERAMICS INTERNATIONAL
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2023
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IF 5.2
Tingting Tang,Hua Huang,Chaoyang Li,Jian Shen
High performance and miniaturization are becoming increasingly important for practical microwave electronics and high-density communication systems. Here, LiNb 0.6 Ti 0.5- x (Zn 1/3 Nb 2/3 ) x O 3 (LNT- x ZN, x = 0, 2, 4, 6, 8 mol%) ceramics have been successfully prepared by a solid-phase reaction. The relationship between the physical structure, microscopic morphology, Raman spectroscopy , and microwave properties is revealed. The better microwave dielectric properties of the LNT-4ZN ceramic sintered at 1075 °C are ε r ∼59.9, Q× f ∼8261 GHz, and τ f ∼-7.4 ppm/°C. Using this ceramic, a miniaturized dielectric resonant antenna (DRA) is designed and demonstrated. The return loss, radiation efficiency, and realized gain of this device at the center frequency are −43.57 dB, 78.4 %, and 8.59 dB, respectively. The antenna, in addition to the good radiation performance, has a size advantage over similar devices (#Cylindrical sample, # R 3.1 mm × h 1.6 mm, @Square substrate, @ a = b = 18 mm × h 3.1 mm). This work exemplifies the great potential of LNT-4ZN materials in communication devices and promotes the application of microwave dielectric ceramics in antenna fields.
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JOURNAL OF ORGANIC CHEMISTRY
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2023
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IF 3.6
Yuan Li,Jiamei Shen,Yawei Shen,Yanfeng Li,Kai Luo,Lei Wu
A novel and efficient tandem SN2 nucleophilic substitution/Dieckmann condensation reaction of α-iodomethyl phosphine oxide with methyl thiosalicylate derivatives has been developed by using NaOH as a base, which enables the expeditious synthesis of 2-phosphonyl-3-hydroxybenzo[b]thiophene derivatives in moderate to high yields under simple conditions. This research provides not only a convenient method for the functionalization of benzo[b]thiophenes at the 2-position and 3-position but also new organophosphorus molecules. Furthermore, several new phosphonyl-substituted benzo[b]thiophenes were obtained from the resultant 2-phosphonyl-3-hydroxybenzo[b]thiophenes.
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JOURNAL OF MOLECULAR STRUCTURE
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2023
·
IF 3.8
JiongYa Tang,Wen Lu,Jiayi Hu,Yuqi Jia,Xuanyuxiang He,Lin Li,Shilong Yang,Yanqin Wang,Li Xu
The azobenzene coumarin derivatives 2 – 10 , in which the coumarin moiety is linked to substituted phenyl and pyridine groups via amide bonds, and a copper complex with compound 8 ( 8-CuCl 2 ) were designed and synthesized, and their anticancer activities were investigated. Compounds 2–10 and 8-CuCl 2 exhibited different degrees of anticancer activities against four cancer cell lines (HeLa, A549, MCF-7, and HepG-2). Among them, compound 6 exhibited stronger cytotoxicity (IC 50 = 0.51 ± 0.22 μM) against A549 cell lines and was less toxic to normal cells than Doxorubicin (DOX) (IC 50 = 1.18 ± 0.03 μM). Compound 8 exhibited stronger cytotoxicity against MCF-7 cell lines than DOX with an IC 50 value 48 times higher than DOX (IC 50 = 0.42 ± 0.23 μM for 8 ; IC 50 = 20.64 ± 3.67 μM for DOX). Meanwhile, compound 8 was much less toxic to normal human umbilical vein endothelial cells (HUVEC) cells than DOX with a 3000 times higher selectivity index (SI) (SI > 238.10 for 8 ; SI = 0.078 for DOX). The results of cell apoptosis and cycle assays showed that compound 6 induced apoptosis in A549 cells more considerably and blocked cells in the S phase, whereas compound 8 induced late apoptosis in MCF-7 cells and blocked cells in the S phase. Ultraviolet and fluorescence spectroscopy analyses revealed that compounds 6 and 8 bound to deoxyribonucleic acid (DNA) via intercalation. In summary, compound 8 was developed as a potential and effective cytotoxicity against MCF-7 cell lines worthy of further investigation.
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MATERIALS & DESIGN
·
2021
·
IF 7.991
Xuesong Zhang,Yuguang Li,Changxiang Li,Fan Yang,Zhengming Jiang,Liyan Xue,Zhiheng Shao,Zhigang Zhao,Meiying Xie,Shuwen Yu
In this study, a new type of (La 0.2 Ce 0.2 Gd 0.2 Er 0.2 Tm 0.2 ) 2 (WO 4 ) 3 single-phase high-entropy ceramic (HEC) powder was designed, prepared by solid-phase synthesis, and evenly mixed into an epoxy resin (EP) matrix to test the thermal neutron and γ-ray shielding performance. In terms of γ-ray shielding, (La 0.2 Ce 0.2 Gd 0.2 Er 0.2 Tm 0.2 ) 2 (WO 4 ) 3 showed a higher lead equivalent value than EP at 65 keV, indicating a clear shielding effect in the feeble absorbing area of lead-based and bismuth-based materials; moreover, (La 0.2 Ce 0.2 Gd 0.2 Er 0.2 Tm 0.2 ) 2 (WO 4 ) 3 showed good γ-ray shielding performance in both low-energy and medium-energy regions. In terms of thermal neutron shielding, the composite with the highest HEC content (EP/W3) had a nearly 100% shielding efficiency, while that of EP was approximately 50%, indicating that this material has favorable thermal neutron and γ-ray shielding performance. Moreover, the thermal conductivity of the resulting composite material was lower than 0.3 W·m −1 ·K −1 , the tensile strength was higher than 10 MPa, and the density was lower than 1.5 g·cm −3 . All these results suggest that (La 0.2 Ce 0.2 Gd 0.2 Er 0.2 Tm 0.2 ) 2 (WO 4 ) 3 is a candidate radiation shielding material.
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Materials Chemistry Frontiers
·
2021
·Vol. 5
·期 12
·4645-4657
·
IF 6.482
Xiangxin Tian,Zhaoxing Hu,Zeliang Gao,Yongzhuan Zhang,Chuanming Li,Hongwei Qi,Xiuping Liu,Rongkun Zheng,Jiangtao Xu,Jingquan Liu
The quasi two-dimensional Ruddlesden–Popper perovskites (RPPs) have drawn unprecedented research attention due to their superior long-term environmental stability, abundant structural diversity, and favorable performance in energy-related application scenarios. Rational molecular design strategies, especially proper selections and modifications on the bulky organic spacer cations, play a vital role in obtaining RPPs with desired properties. Recently, employing fluorinated organic cations for further improving the stability and artificial tuning of the performance of RPP based devices has become a promising strategy. However, the mechanism of how fluorination affects the orientation of the spacer cations and the interactions between the organic slabs and the inorganic frameworks is still controversial and needs further investigations, especially on the structure–property relationship based on well-developed single crystals. Herein, we adopted meta-fluorophenethylamine (3-FPEA) as the spacer cation and successfully synthesized a RPP, (3-FPEA)2PbI4. Centimeter-sized single crystals of this material were grown through the bottom-seeded solution growth (BSSD) method by using hydroiodic acid as the self-solvent. (3-FPEA)2PbI4 exhibits superior thermal stability (from −175 °C to 281 °C), while a reversible phase transition occurs at 212 °C and it remains stable for at least 90 days when exposed to RH 80% at room temperature. Structural refinement and optical characterization indicate that the meta-substitution of fluorine breaks its original symmetry from monoclinic Cc to triclinic P space group accompanying a certain degree of disorder of the Pb2+ ions as well as the equatorial bridging I− ions and leads to a smaller band gap (2.20 eV), blue-shifted photoluminescence peak (516 nm), and longer decay time (τave = 1.36 ns). This work offers further insights into the structure–property relationships of the fluorinated RPPs and provides an effective strategy for designing novel RPPs with superior photoelectric properties.
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FOOD CHEMISTRY
·
2021
·
IF 7.514
Ye Yuan,Fangmin Xu,Min Jin,Xuexi Wang,Xiaoying Hu,Mingming Zhao,Xin Cheng,Jiaxiang Luo,Lefei Jiao,Mónica B. Betancor,Douglas R. Tocher,Qicun Zhou
While tissue fatty acid compositions reflect that of the dietary lipid source, little information is available on how dietary oils modify lipid class and molecular species profiles in hepatopancreas of crustacean. Herein, an 8-week nutritional trial and untargeted lipidomic analysis were used to investigate the impacts of dietary n-3 PUFA lipid sources including fish oil, krill oil and linseed oil on the lipidomic characteristics of hepatopancreas of swimming crab ( Portunus trituberculatus ). Dietary krill oil significantly increased distribution of 20:5n-3 and 22:6n-3 at sn-2 in phosphatidylcholine and phosphatidylethanolamine compared to fish oil. Fish oil intake promoted the deposition of 20:5n-3 and 22:6n-3 at sn-1,2,3 in triglyceride compared to linseed oil, which significantly increased the specific accumulation of 18:3n-3 at sn-1,3 in triglyceride and sn-2 in phosphatidylcholine and phosphatidylethanolamine. The study revealed metabolic responses to different dietary n-3 PUFA in swimming crab, which provided novel insight into the lipid nutrition of crustacean.
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CHEMISTRY & BIODIVERSITY
·
2021
·Vol. 18
·期 5
·e2100128
·
IF 2.408
Shu-Hua Zhang,Jiewei Yang,Hao Ma,Yu Yang,Guo-Feng Zhou,Xue Zhao,Rui Xu,Dan Nie,Guo-Gang Zhang,Jun-Jie Shan,Cheng-Bin Cui,Chang-Wei Li
Five new peptaibols, longibramides A–E ( 1 – 5 ) with 11 amino acid residues, were isolated from a fungus Trichoderma longibrachiatum Rifai DMG-3-1-1, which was isolated from a mushroom Clitocybe nebularis (Batsch) P. Kumm collected from coniferous forest in the subboreal area of northeast China. The structures of longibramides A–E were determined by their spectroscopic data (NMR and MS-MS spectra), their absolute configurations were determined by X-ray diffractions and Marfey's analyses. The X-ray diffractions of longibramides A, B, and the similar CD spectra of A–E showed that they all had α -helix conformations. Longibramides B and E showed moderate cytotoxicities against BV2 and MCF-7 cells and also showed some inhibitory effects against methicillin-resistant Staphylococcus aureus MRSA T144. L- trans- Hyp was not commonly found in natural peptaibols, which was the 6 th or 10 th amino acid residue in longibramides C–E. The X-ray diffractions of longibramides A and B afforded the accuracy conformations of their secondary structures, which maybe help to interpret the structure-activity relationships of the family of peptaibols in the future. Graphical
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CHEMICAL ENGINEERING JOURNAL
·
2021
·
IF 13.273
Qinxue Yang,Ying Yan,Xiaofang Yang,Guiying Liao,Jie He,Dongsheng Wang
The possible effect of complexation of tetracycline (TC) with metal ions on the degradation of TC by homogeneous activated peroxymonosulfate (PMS) was investigated. The oxidation kinetics of TC indicated the differences in PMS activation ability by Fe 2+/3+ and Ru 3+ . Fe 2+/3+ could activate PMS to generate HO• and SO 4 - • as is known, while Ru 3+ promoted the generation of 1 O 2 from PMS, though 1 O 2 may be not the only and dominant oxidant. The stronger complex ability of Ru 3+ and Fe 3+ with TC than Fe 2+ contributed to the enhanced oxidation of TC in Fe 3+ /PMS and Ru 3+ /PMS systems. The complexation facilitated TC degradation possibly due to the electron reconfiguration of metal ions and TC, such as reduce the stability of -C–C- double bands in TC structures and made it more vulnerable. The complexation reactions were commonly occurred but ignored in metal species activated PMS systems, the findings in this study suggested that the interaction between metal ions and organic contaminants should be reconsidered and utilized in the development of AOPs.
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SCIENCE OF THE TOTAL ENVIRONMENT
·
2021
·
IF 7.963
Changsong Li,Yijing Li,Qiang Li,Junling Duan,Juying Hou,Qin Hou,Shiyun Ai,Houshen Li,Yuechao Yang
Phosphates and organophosphorus cause environmental pollution , and excessive phosphate leads to water eutrophication . Glyphosate , an organophosphorus herbicide, harms the environment and human health. In this study, regenerable magnetic AL/Fe 3 O 4 /La(OH) 3 adsorbents were developed by modifying Fe 3 O 4 and La(OH) 3 on aminated lignin (AL) for phosphate and glyphosate removal. The adsorption capacity for phosphate and glyphosate reached 60.36 mg g −1 and 83.87 mg g −1 when the initial concentrations were 150 mg L −1 and 250 mg L −1 , respectively. The thermodynamic data showed that adsorption is a spontaneous and endothermic process. Adsorption can be applied at pH values ranging from 3 to 11 and is more suitable under acidic conditions. Fe 3 O 4 and La(OH) 3 both enhanced the adsorption capacities of phosphate and glyphosate. Phosphate and glyphosate compete slightly when coexisting in the adsorption process at low concentrations. Due to the magnetic properties of Fe 3 O 4 , the adsorbents can be separated rapidly and effectively with an external magnetic field. 89% adsorption capacity remained after four adsorption-desorption recycles. Thus, AL/Fe 3 O 4 /La(OH) 3 shows potential for phosphate and glyphosate removal as an effective and reusable adsorbent.
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