EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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2014
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IF 3.432
Shengrong Liao,Xiaochu Qin,Ding Li,Zhengchao Tu,Jinsheng Li,Xuefeng Zhou,Junfeng Wang,Bin Yang,Xiuping Lin,Juan Liu,Xianwen Yang,Yonghong Liu
Non-protected 2,5-diketopiperazine derivatives have poor solubility thus with negative impact on their bioavailability. In the present study, twenty-one novel soluble mono-protected, and three non-protected 2,5-diketopiperazine derivatives were designed and synthesized. Their anticancer activity to ten cell lines were evaluated by using CCK8 assay, and the results showed that about half of the mono-protected derivatives had broad-spectrum anticancer activity. Among allyl-protected derivatives, compound 4m had strong activity to all the cell lines (IC 50 = 0.5–4.5 μM), especially to the cancer cell lines U937 (IC 50 = 0.5 μM) and K562 (IC 50 = 0.9 μM). Compound 4m could become a lead compound for further development for anticancer agents .
研究领域:
药物化学
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肿瘤学
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DOI
PubMed
高影响因子
TRANSACTIONS OF TIANJIN UNIVERSITY
·
2012
·Vol. 18
·期 5
·315-319
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IF 0
Feng Yakai,Chen Chengbin,Zhang Li,Tian Hong,Yuan Wenjie
A series of novel copolymers were successfully synthesized by ring-opening polymerization (ROP) of 3(S)-methyl-morpholine-2,5-dione (MMD) and 5-methyl-5-benzyloxycarbonyl-1,3-dioxan-2-one (MBC) using stannous octoate as catalyst. The copolymers were characterized by means of 1H-NMR and FT-IR spectroscopy. Gel permeation chromatography (GPC) test shows that the average-number relative molecular mass and average-weight relative molecular mass slightly increase with the increase of MBC content in feed. The results of differential scanning calorimetry (DSC) demonstrate that the glass transition temperature of copolymers increases with the increase of MBC content in copolymers. The copolymers of MMD and MBC are amorphous copolymers, as indicated by DSC results, while the homopolymer of MMD is semicrystalline.
研究领域:
高分子化学
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材料科学
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产品关联
DOI
SCIENCE OF THE TOTAL ENVIRONMENT
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2021
·
IF 7.963
Ji Liu,Wei Zhao,Shuang-wei Yang,Bin Hu,Ming-xin Xu,Shan-Wei Ma,Qiang Lu
Incineration of food waste leads to the release of NO x pollutants, whereas the formation mechanism of the NO x precursors (HCN, NH 3 , and HNCO) during the initial pyrolysis process is far from well-studied, limiting the source control on NO x release. In this work, 2,5-diketopiperazine (DKP) was selected as the N-containing model compound to study the formation mechanism of NO x precursors in food waste pyrolysis, by combining experiments and density functional theory (DFT) calculations. The C1-N2 bond broken via the N2-to-N5 H-transfer possesses the lowest energy barrier, together with the largest reaction rate constants in the range of 400–800 °C. NH 3 can be easily generated with low energy barriers and high rate constants at low temperatures (below 630 °C). Whereas, the rate constants of the pathways for HCN formation will exceed those for NH 3 generation in the range of 630–740 °C. In addition, the DKP pyrolysis can also lead to the formation of HNCO with a very low energy barrier, and it can convert into HCN and NH 3 through further hydrogenation and decomposition. These calculation results are exactly consistent with the experimental results that NH 3 was the main precursor in the range of 400–600 °C, and the yield of HCN exceeded that of NH 3 when the temperature was over 600 °C. Our current work on the formation mechanism of NO x precursors during the pyrolysis of DKP can provide theoretical guidance for the development of NO x control technology in the pyrolysis/combustion process of organic waste.
研究领域:
环境科学
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化学工程
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能源科学
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DOI
PubMed
高影响因子
RSC Advances
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2015
·Vol. 5
·期 63
·51020-51026
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IF 3.84
Shengrong Liao,Ying Xu,Yong Tang,Junfeng Wang,Xuefeng Zhou,Liang Xu,Yonghong Liu
A small library of soluble 2,5-diketopiperazine derivatives were designed, synthesized and evaluated as antifouling agents against two species of marine organisms: Balanus amphitrite and Bugula neritina by larval attachment assay. The results showed that different derivatives had different antifouling activities. Among these compounds, 3a (EC50 = 2.5 μg mL−1), 3b (EC50 = 3.2 μg mL−1) and 3d (EC50 = 1.6 μg mL−1) had strong activities, and 2d (EC50 = 20.5 μg mL−1), 3l (EC50 = 25.0 μg mL−1) and 3m (EC50 = 18.5 μg mL−1) had moderate activities against Balanus amphitrite, but other compounds had no activities. Differently, compounds 3d (EC50 = 3.1 μg mL−1) and 3i (EC50 = 2.3 μg mL−1) exhibited strong activities, and 3a (EC50 = 11.3 μg mL−1) and 3c (EC50 = 17.2 μg mL−1) showed moderate activities against Bugula neritina, whereas other compounds had no activities. All of the active compounds had stronger antifouling activities than those of the natural product cyclo-(L-Phe-L-Pro). Compound 3d could be a new template molecule for further development as an antifouling agent because of its strong inhibitory activities against both species of fouling organisms with low or no toxicity to the environment.
研究领域:
海洋生物学
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药物化学
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环境科学
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DOI
高影响因子
ORGANIC & BIOMOLECULAR CHEMISTRY
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2022
·Vol. 20
·期 15
·3201-3210
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IF 3.89
Lin Chen,Wei Liang
Michael/ammonolysis cascade reactions between cyclohexane-1,3-dione-derived enaminones and olefinic azlactones via phase-transfer catalysis have been developed. This method provides rapid access to a suite of architecturally complex and diverse quinoline-2,5-diones bearing a secondary amide group at the C-3 position in moderate to excellent yields (53–94%) and with excellent diastereoselectivities (>99 : 1 dr in most cases). The achievement of a preparative-scale reaction and the diverse product derivatization that can be obtained highlight the application potential of this protocol both in academic and industrial settings. An investigation of the reaction mechanism implies that tetrabutylammonium hydroxide may be the actual catalyst during this cascade reaction.
研究领域:
有机化学
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药物化学
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DOI
高影响因子
JOURNAL OF HETEROCYCLIC CHEMISTRY
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2011
·Vol. 48
·期 6
·1434-1439
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IF 0.962
Qiang Shao,Hui Liu,Ting-Ting Wang,He-Ping Zeng
Several 3,3′-(1,4-phenylene)bis(1,5-diones) and their chalcone precursors have been prepared in good to excellent yield via aldol addition and Michael addition starting from 3-acetyl-2,5-dimethylfuran or 3-acetyl-2,5-dimethyl-thiophene with terephthalaldehyde in the presence of appropriate base NaOH or lithium diisopropylamide. The kind and amount of alkali played a critical role in improving the reaction rates and yields of the products. J. Heterocyclic Chem., (2011).
研究领域:
有机化学
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合成化学
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DOI
高影响因子
JOURNAL OF SOLID STATE ELECTROCHEMISTRY
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2021
·Vol. 25
·期 6
·1847-1859
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IF 2.647
Li Chunxia,Guo Xin,Du Hongmei,Zhao Jinsheng,Liu Lixia,Yuan Qing,Fu Chonggang
Two novel donor-acceptor (D-A)-conjugated polymers, poly[(thiophene-2,5-yl)-((benzo[1,2-b:6,5-b′]dithiophene-4,5-dione)-2,7-yl)] (PTDT) and poly[((2,3-dihydrothieno[3,4-b] [ 1 , 2 ]dioxine)-5,7-diyl)-((benzo[1,2-b:6,5-b′]dithiophene-4,5-dione)-2,7-diyl)] (PTDO), have been synthesized with the same acceptor unit of benzo[1,2-b:6,5-b′]dithiophene-4,5-dione and different donor units of thiophene (Th) and 3,4-ethylenedioxothiphene (EDOT), respectively. And then, two composites (PTDT@C and PTDO@C) are made by coating the polymers on the surface of active carbon with an in situ method, which are used as the electrode materials of lithium-ion battery. The reversible capacities of PTDT@C and PTDO@C are 246.9 and 322.3 mAh g −1 at 0.1 A g −1 after 300 cycles running, respectively. By deducing the capability contribution of pure carbon, the theoretical capacities of the pure polymers are calculated to be 596 and 991 mAh g −1 , respectively, for PTDT and PTDO, which correspond to the lithium storage number of 6.7 and 13.3, respectively, for the least repeating unit of the polymers. With the help of theoretical calculations, the underlying mechanisms for the different electrochemical performances of the polymers are discussed and revealed. The structure-activity relationship discussed in this work may provide the design principle for the construction of the D-A-type polymers used as high-capacity electrode materials for organic rechargeable batteries.
研究领域:
材料科学
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电化学
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产品关联
DOI
高影响因子
Journal of CO2 Utilization
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2022
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IF 8.321
Jiqing Dong,Ran Ping,Xun Dai,Dongchao Wang,Fusheng Liu,Shanshan Du,Mengshuai Liu
The combination of pyrrolidine-2,5-dione-derived ionic liquids with silver acetate (AgOAc) were developed as binary catalysts for conversion of simulated flue gas CO 2 and propargylic alcohols to α-alkylidene cyclic carbonates . By tuning different catalyst components, the [HTMG][Pyrro]/AgOAc system was confirmed to be the most efficient and exhibited an excellent synergistic action in facilitating the carboxylic cyclization under room temperature and solvent-free conditions. The influence of reaction parameters on carboxylic cyclization of CO 2 with 2-methylbut-3-yn-2-ol were optimized. Under the determined conditions, the [HTMG][Pyrro]/AgOAc system was stable enough to show durable high activity in eight recycles, and also versatile in carboxylic cyclization of flue gas CO 2 with other propargylic alcohols. Moreover, a thorough comparison of [HTMG][Pyrro]/AgOAc with the reported catalysts was provided and evaluated, the results suggested that the developed catalytic system has significant advantages in practical application. Finally, the mechanistic details for the conversion of CO 2 into α-alkylidene cyclic carbonates catalyzed by [HTMG][Pyrro]/AgOAc was also elucidated on the basis of reactants activation.
研究领域:
化学
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催化
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环境科学
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材料科学
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）