EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
·
2014
·Vol. 2014
·期 34
·7572-7576
·
IF 3.154
Lijing Fang,Chunlei Wu,Zaidan Yu,Peng Shang,Yongxian Cheng,Yuefeng Peng,Wu Su
Graphical A highly efficient protocol for the triphosgene-mediated solid-phase coupling of proteinogenic amino acids is developed and applied to the first total synthesis of the bioactive natural octacyclopeptide brachystemin A. A reproducible, highly efficient, and racemization-free protocol for the triphosgene-mediated solid-phase coupling of proteinogenic amino acids was developed. The efficiency of the reaction was demonstrated by the first total synthesis of the bioactive natural octacyclopeptide brachystemin A. This protocol will broaden the application of triphosgene in the synthesis of a wide range of peptides, including aromatic amino acids, N -alkylated amino acids, as well as proteinogenic amino acids.
研究领域:
有机化学
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药物化学
·
生物合成
✓ 已验证
DOI
高影响因子
INDUSTRIAL & ENGINEERING CHEMISTRY RESEARCH
·
2014
·
IF 2.235
Xiuzhen Wei,Songxue Wang,Yingying Shi,Hai Xiang,Jinyuan Chen
A positively charged, composite, hollow-fiber nanofiltration (NF) membrane was fabricated by interfacial polymerization using polyethylenimine and trimesoyl chloride as reactive monomers. Rejection rates of different salts and dyes were measured by the NF membranes at various pH values. The effects of dye and salt concentrations on the membrane performance for dye purification were investigated. The dye and salt rejection rates would gradually decrease with an increase in the dye and salt concentrations. Then the influence of the volume concentration factor on dye purification during constant volume batch diafiltration process was studied. The results indicated that the higher of the concentration factor was, the better the concentration effect would be, and the less time would be needed.
研究领域:
材料科学
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环境工程
·
化学工程
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF ORGANIC CHEMISTRY
·
2018
·
IF 4.805
Zhen-Hua Li,Zhi-Jiang Jiang,Qiao-Ling Shao,Jin-Jing Qin,Qiang-Feng Shu,Wen-Hao Lu,Wei-Ke Su
A one-pot cascade heterocyclization strategy has been developed for the synthesis of 2,4-dichloro-substituted pyrano[2,3-d]pyrimidines and furo[2,3-d]pyrimidines from linear γ- and β-ketomalononitriles using triphosgene and triphenylphosphine oxide. The reaction afforded synthetic useful products with moderate to good yields, bypassing the conventional harsh conditions of chlorination. The mechanistic study revealed that the reaction proceeded with a non-isocyanate route, and the second step may conduct in a triphenylphosphine oxide-catalyzed manner.
研究领域:
有机化学
·
药物化学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF HETEROCYCLIC CHEMISTRY
·
2023
·
IF 2.4
Ping Zhao,Qingle Zeng
We have developed a diversity-oriented, substrate-controlled, chemoselective synthetic method for a variety of structurally diverse 1-sulfonylquinazoline-2,4(1H,3H)-diones and 2-sulfonamidobenzonitriles. This substrate-controlled synthesis is accomplished through the condensation reaction of 2-(sulfonamido)benzamides with or without an N-methyl group on the amides. The reactions are fulfilled within half an hour at room temperature with solid triphosgene as a convenient condensing agent and pyridine as an acid acceptor. This protocol features easily available starting materials, mild reaction conditions, easy experimental operation, and moderate to excellent yields of products.
研究领域:
有机化学
·
药物化学
✓ 已验证
DOI
高影响因子
RESEARCH ON CHEMICAL INTERMEDIATES
·
2022
·Vol. 49
·期 1
·241-252
·
IF 3.134
Xing Qianqian,Zhao Jiancheng,Zhu Yulei,Hou Xianglin,Wang Yingxiong
5-Chloro-2-pentanone (5C2P) and its derivatives are widely utilized in the pharmaceutical and agrochemical industry. A new catalytic approach was proposed to convert 3-acetyl-1-propanol to 5C2P using bis(trichloromethyl)carbonate (triphosgene, BTC) as the efficient chlorine source. Various qualitative and quantitative nuclear magnetic resonance techniques ( 1 H, 13 C NMR), especially 1D selective gradient total correlation spectroscopy (Sel-TOCSY) and 2D heteronuclear single quantum correlation ( 1 H- 13 C HSQC) were used in the process. The reaction conditions, such as temperature, time, mole ratio, solvent as well as initiator were optimized. Experiment results showed that the yield of 5C2P reached a maximum of 97.93% in 1,2-dichloroethane at 80 °C after 2 h under the initiation of N,N-dimethylacetamide, and the optimal molar ratio of 3-acetyl-1-propanol to BTC was 1:0.4. The reaction mechanism was proposed and confirmed accordingly. Interestingly, an intermediate product of 1-(dimethylamino)ethyl carbonochloridate was observed, and its chemical structure was characterized by both Sel-TOCSY and 1 H- 13 C HSQC. This study enriched the catalytic reaction ways for the preparation of 5C2P.
研究领域:
有机化学
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药物化学
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合成化学
✓ 已验证
产品关联
DOI
高影响因子
Nature Communications
·
2024
·Vol. 15
·期 1
·1-14
·
IF 14.7
Peng Chuan,Zhu Yuling,Zhang Kaibo,Wang Yiwei,Zheng Yi,Liu Yang,Fu Weili,Tan Hong,Fu Qiang,Ding Mingming
Nonaromatic and nonconjugated fluorescent materials have garnered increasing attention in recent years. However, most non-classical chromophores are derived from electro-rich nitrogen and oxygen atoms, which suffer from short emission wavelengths, low efficiency, limited responsiveness, and obscure luminescence mechanisms. Here we present an emission mechanism in bioactive polycysteine, an aliphatic polymer that displays polymerization- and aggregation-induced emission, high quantum yield, and multicolor emission properties. We show that the hydrogen atoms bonded to the sulfur atoms play a crucial role in luminescence. This enables reversible modulation of polymer fluorescence under reducing and oxidizing conditions, facilitating specific imaging and quantitative detection of redox species in cells and in vivo. Furthermore, the polymer exhibits better anti-inflammatory and antioxidative activities compared to first-line clinical antioxidants, offering a promising platform for in vivo theragnosis of diseases such as osteoarthritis.
研究领域:
材料科学
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生物医学工程
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化学
·
生物学
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药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMACROMOLECULES
·
2024
·
IF 5.5
Hao Zhang,Chengyuan Xing,Binyuan Yan,Hanqi Lei,Yupeng Guan,Shiqiang Zhang,Yang Kang,Jun Pang
Combination therapy has emerged as a promising approach for treating tumors, although there is room for improvement. This study introduced a novel strategy that combined the enhancement of apoptosis, ferroptosis, and DNA damage to improve therapeutic outcomes for prostate cancer. Specifically, we have developed a supramolecular oxidative stress nanoamplifier, which was comprised of β-cyclodextrin, paclitaxel, and ferrocene-poly(ethylene glycol). Paclitaxel within the system disrupted microtubule dynamics, inducing G2/M phase arrest and apoptosis. Concurrently, ferrocene utilized hydrogen peroxide to generate toxic hydroxyl radicals in cells through the Fenton reaction, triggering a cascade of reactive oxygen species expansion, reduction of glutathione levels, lipid peroxidation, and ferroptosis. The increased number of hydroxyl radicals and the inhibitory effect of THZ531 on DNA repair mechanisms exacerbated DNA damage within tumor cells. As expected, the supramolecular nanoparticles demonstrated excellent drug delivery ability to tumor cells or tissues, exhibited favorable biological safety in vivo, and enhanced the killing effect on prostate cancer.
研究领域:
药理学
·
肿瘤学
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纳米医学
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生物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
SENSORS
·
2025
·Vol. 25
·期 2
·407
·
IF 3.5
Yingzhen Zhang,Jun Xiao,Ruiying Peng,Xueliang Feng,Haimei Mao,Kunming Liu,Zhenzhong Liu,Chunxin Ma
The detection of highly toxic chemicals such as phosgene is crucial for addressing the severe threats to human health and public safety posed by terrorist attacks and industrial mishaps. However, timely and precise monitoring of phosgene at a low cost remains a significant challenge. This work is the first to report a novel fluorescent system based on the Intramolecular Charge Transfer (ICT) effect, which can rapidly detect phosgene in both solution and gas phases with high sensitivity by integrating a benzo[1,2-b:6,5-b’]dithiophene-4,5-diamine (BDTA) probe. Among existing detecting methods, this fluorescent system stands out as it can respond to phosgene within a mere 30 s and has a detection limit as low as 0.16 μM in solution. Furthermore, the sensing mechanism was rigorously validated through high-resolution mass spectrometry (HRMS) and density functional theory (DFT) calculations. As a result, this fluorescent probing system for phosgene can be effectively adapted for real-time, high-sensitivity sensing and used as a test strip for visual monitoring without the need for specific equipment, which will also provide a new strategy for the fluorescent detection of other toxic materials.
研究领域:
化学
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环境科学
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毒理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Advanced Healthcare Materials
·
2024
·
IF 10
Yixuan Xu,Huiping Dang,Changchang Teng,Dalong Yin,Lifeng Yan
Rapid propagation of tumor cells requires plenty of energy, which is adenosine triphosphate (ATP) dependent. ATP inhibition in tumors not only results in the starvation of tumor cells but also down-regulation of the level of heat shock proteins (HSPs), which usually increase during traditional photothermal therapy (PTT), especially when the temperature is up 50 °C. 2-deoxy-D-glucose (2DG) is an anti-glycolytic reagent and can be used as an efficient agent for ATP inhibition in tumors. Compared with typical PTT, low-temperature mild photothermal therapy (MPTT) is receiving more and more attention because it avoids the high temperatures causing damage to the normal tissue, and the increase of HSPs which decrease PTT. Here, multifunctional polypeptide nanoparticles pDG@Ahx conjugating both a NIR probe Ahx-BDP and 2DG into the side chain of the amphiphilic polypeptide have been prepared. In vitro and in vivo studies reveal that the as-prepared nanoparticles achieve a synergistic effect of starvation/MPTT/PDT (photodynamic therapy), and it provides a new strategy to NIR-I/II fluorescence imaging-guided starvation/MPTT/PDT synergy therapy for tumors.
研究领域:
生物医学工程
·
肿瘤学
·
纳米医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Materials Chemistry B
·
2024
·
IF 6.1
Junwei Yang,Xianzhen Dong,Wenying Wei,Kun Liu,Xiaopei Wu,Honglian Dai
The healing of scalded wounds faces many challenges such as chronic inflammation, oxidative stress, wound infection, and difficulties in vascular and nerve regeneration. Treating a single problem cannot effectively coordinate the complex regenerative microenvironment of scalded wounds, limiting the healing and functional recovery of the skin. Therefore, there is a need to develop a multi-effect treatment plan that can adaptively address the issues at each stage of wound healing. In this study, we propose a scheme for on-demand release of hydrogen sulfide (H2S) based on the concentration of reactive oxygen species (ROS) in the wound microenvironment. This is achieved by encapsulating peroxythiocarbamate (PTCM) in the ROS-responsive polymer poly(ethylene glycol)–poly(L-methionine) (PMet) to form nanoparticles, which are loaded into a thermosensitive injectable hydrogel, F127-poly(L-aspartic acid-N-hydroxysuccinimide) (F127-P(Asp-NHS)), to create a scald dressing. The H2S released by the hydrogel dressing on demand regulates the wound microenvironment by alleviating infection, reducing oxidative stress, and remodeling inflammation, thereby accelerating the healing of full-thickness scalded wounds. This hydrogel dressing for the adaptive release of H2S has great potential in addressing complex scalded wounds associated with infection and chronic inflammation.
研究领域:
材料科学
·
生物医学工程
·
伤口愈合
·
药学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMACROMOLECULES
·
2024
·
IF 5.5
Qiang Cheng,Weixing Wang,Xianzhen Dong,Yunhui Chai,Takashi Goto,Rong Tu,Lesan Yan,Aixi Yu,Honglian Dai
The multifaceted process of nerve regeneration following damage remains a significant clinical issue, due to the lack of a favorable regenerative microenvironment and insufficient endogenous biochemical signaling. However, the current nerve grafts have limitations in functionality, as they require a greater capacity to effectively regulate the intricate microenvironment associated with nerve regeneration. In this regard, we proposed the construction of a functional artificial scaffold based on a “two-pronged” approach. The whole system was developed by encapsulating Tazarotene within nanomicelles formed through self-assembly of reactive oxygen species (ROS)-responsive amphiphilic triblock copolymer, all of which were further loaded into a thermosensitive injectable hydrogel. Notably, the hydrogel exhibits obvious temperature sensitivity at a concentration of 6 wt %, and the nanoparticles possess concentration-dependent H2O2-response capability with a controlled release profile in 48 h. The combined strategy promoted the repair of injured peripheral nerves, attributed to the dual role of the materials, which mainly involved providing structural support, modulating the immune microenvironment, and enhancing angiogenesis. Overall, this study opens up intriguing prospects in tissue engineering.
研究领域:
组织工程
·
神经科学
·
生物材料
·
药物递送系统
·
再生医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Science Bulletin
·
2024
·
IF 18.8
Shijie Li,Sarun Juengpanich,Win Topatana,Tianao Xie,Lidan Hou,Yiyuan Zhu,Jiadong Chen,Yukai Shan,Yina Han,Ziyi Lu,Tianen Chen,Charlie Topatana,Bin Zhang,Jiasheng Cao,Jiahao Hu,Jiafei Yan,Yingxin Chen,Zhen Gu,Jicheng Yu,Xiujun Cai,Mingyu Chen
Adavosertib (ADA) is a WEE1 inhibitor that exhibits a synthetic lethal effect on p53-mutated gallbladder cancer (GBC). However, drug resistance due to DNA damage response compensation pathways and high toxicity limits further applications. Herein, estrone-targeted ADA-encapsulated metal–organic frameworks (ADA@MOF-EPL) for GBC synthetic lethal treatment by inducing conditional factors are developed. The high expression of estrogen receptors in GBC enables ADA@MOF-EPL to quickly enter and accumulate near the cell nucleus through estrone-mediated endocytosis and release ADA to inhibit WEE1 upon entering the acidic tumor microenvironment. Ultrasound irradiation induces ADA@MOF-EPL to generate reactive oxygen species (ROS), which leads to a further increase in DNA damage, resulting in a higher sensitivity of p53-mutated cancer cells to WEE1 inhibitor and promoting cell death via conditional synthetic lethality. The conditional factor induced by ADA@MOF-EPL further enhances the antitumor efficacy while significantly reducing systemic toxicity. Moreover, ADA@MOF-EPL demonstrates similar antitumor abilities in other p53-mutated solid tumors, revealing its potential as a broad-spectrum antitumor drug.
研究领域:
肿瘤学
·
药学
·
纳米技术
·
癌症生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）