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Design, Synthesis and Biological Activities of N-（Furan-2-ylmethyl）-lH-indole-3-carboxamide Derivatives as Epidemal Growth Factor Receptor Inhibitors and Anticancer Agents

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Chemical Research in Chinese Universities 2017年第3期33卷 365-372页

作者： ZHANG Lan DENG Xinshan WU Jiaofeng meng guangpeng LIU Congchong CHEN Guzhou ZHAO Qingchun HU Chun Key Laboratory of Structure-based Drug Design & Discovery Ministry of Education Shenyang Pharmaceutical University Shenyang 110016 P. R. China Department of Pharmacy General Hospital of Shenyang Military Area Command Shenyang 110016 P. R. China

A series ofN-（furan-2-ylmethyl）-lH-indole-3-carboxamide derivatives（6a--6p） was designed and synthe- sized for developing novel indole scaffolds as anticancer agents targeting the epidemal growth factor receptor （EGFR）, and the cytotoxic activities of the target compounds were evaluated against three EGFR high-expressed cancer cell lines[human lung adenocarcinoma cell line（A549）, Henrietta Lacks strain of cancer cell line（HeLa） and human colorectal cancer cell line（SW480）], one EGFR low-expressed cell line（human liver cancer cell line, HepG2） and one human liver normal cell line（HL7702） using 3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyl tetrazolium bromide （MTT） assay, Some target compounds exhibited potent anficancer activities against A549, HeLa, SW480 and weak activities on HepG2, which signifies that the target compounds are likely to be EGFR inhibitors as expected. And they showed weak cytotoxic effects on HL7702, which implies the target compounds are probably to be of low toxicity against normal cells. Among them, the target compound 1-ethyl-N-（fttran-2-ylmethyl）-5-{2-{ [2-（2-methoxy- phenoxy）ethyl]amino}-2-oxoethoxy}-2-methyl-1H-indole-3-carboxamide（6p） with 2-{[2-（2-methoxyphenoxy）ethyl]- amino}-2-oxoethoxy group at the C5 position of the N-（furan-2-ylmethyl）-lH-indole-3-carboxamide scaffold exhibited the most potent anticancer activity. Also the binding interaction of the target compound 6p with EGFR was explored by molecular docking. Conclusively, the novel indole scaffold may be beneficial to investigate new anticancer agents for targeting the EGFR.

关键词： Anticancer activity Epidemal growth factor receptor(EGFR) inhibitor N-(Furan-2-ylmethyl)-lH-indole-3-carboxamide derivative

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Synthesis and biological evaluation of indole-3-carboxamide derivatives as antioxidant agents

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Chinese Chemical Letters 2019年第12期30卷 2157-2159页

作者： Erfang Huang Lan Zhang Chuying Xiao guangpeng meng Bingqi Zhang Jianshu Hu David Chi-Cheong Wan Qingguo meng Zhe Jin Chun Hu Key Laboratory of Structure-based Drug Design&Discovery Ministry of EducationShenyang Pharmaceutical UniversityShenyang 110016China School of Biomedical Sciences Faculty of MedicineThe Chinese University of Hong KongHong KongChina Department of Pharmacy Yantai UniveristyYantai 264005China

Oxidative stress results in various pathologies and as consequence antioxidant agents have attracted uninterrupted *** this paper,a novel series of indole-3-carboxamide derivatives(6 a-61) were designed and synthesized based on the melatonin structure as novel *** of them were evaluated for the antioxidant activities in vitro against human neuroblastoma SH-SY5 Y cell line using H2 O2 radical scavenging *** target compounds 6 a,6 f and 6 i indicated better activities than the positive control,ascorbic acid,and 6 a exhibited the best antioxidant *** addition,the structureactivity relationships of the target compounds were also preliminarily summarized based on the obtained experimental data.

关键词： Heterocycle Melatonin Indole-3-carboxamide derivatives Synthesis Antioxidant activity Structure-activity relationship

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Excellentπ-Bowl Semiconductors Based on C_(70)Subunit

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CCS Chemistry 2024年第2期6卷 353-364页

作者： meng Chen Yuxiao Duan Xinyue Liu Qian Zhan Hironobu Hayashi Kyohei Matsuo Hiroko Yamada guangpeng Gao Yonghao Zheng Lei Zhang Beijing Advanced Innovation Center for Soft Matter Science and Engineering Beijing University of Chemical TechnologyBeijing 100029 School of Optoelectronic Science and Engineering University of Electronic Science and Technology of China(UESTC)Chengdu 610054 Division of Materials Science Nara Institute of Science and Technology(NAIST)IkomaNara 630-0192 Key Laboratory of Cluster Science of Ministry of Education Beijing Key Laboratory of Photoelectronic/Electrophotonic Conversion MaterialsSchool of Chemistry and Chemical EngineeringBeijing Institute of TechnologyBeijing 100081

As open substructures of fullerenes,aromaticπ-bowls are promising candidates as new organic semiconductors,as well as attractive hosts for *** demonstrate herein the synthesis and characterization of a novel C_(2v)symmetricπ-bowl,pyracyleno[6,5,4,3,2,1-pqrstuv]pentaphene(3).Bowl 3 was equipped with two distinctive reactive sites,allowing for bromination and cross-coupling reactions to readily yield functionalized bowls with two 2,4,6-trimethylphenyl(5)and triethylsilyl(TES)-ethynyl(6)substituents,***-temperature 1H NMR analysis and density functional theory(DFT)calculations indicated bowl-to-bowl inversions of 3,5,and 6 at room *** alternating the substituents,the crystal structures of the threeπ-bowls 3,5,and 6 could be controlled from 1D linear to 1D slipped to 2D herringbone packing motifs,providing insight into the packing behavior ofπ-bowls.1H NMR titration study indicated that the TES-ethynyl substituent enhanced the ability ofπ-bowl to bind C_(70)with an association constant of 2485 M−*** C_(70)molecules withπ-bowls 3 and 6 formed 1:1 complexes,in which C_(70)molecules aggregated into zig-zag and 1D linear arrays,*** hole mobility of 2.3 cm^(2)V^(−1)^s(−1)and electron mobility of 0.16 cm^(2)V^(−1)^s(−1)ofπ-bowl 3 and its complex with C_(70)were demonstrated,respectively,which proved a great value for the development of aromaticπ-bowl semiconductors with tunable properties for organic electronic devices.

关键词： organic semiconductor π-bowl fullerene crystal engineering mobility

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MicroRNA-451 from Human Umbilical Cord-Derived Mesenchymal Stem Cell Exosomes Inhibits Alveolar Macrophage Autophagy via Tuberous Sclerosis Complex 1/Mammalian Target of Rapamycin Pathway to Attenuate Burn-Induced Acute Lung Injury in Rats

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Biomedical and Environmental Sciences 2024年第9期37卷 1030-1043页

作者： Zhigang Jia Lin Li Peng Zhao Guo Fei Shuangru Li Qinqin Song guangpeng Liu Jisong Liu Affiliated Hospital of Jiang nan University Department of Burn and Plastic SurgeryWuxi 214000JiangsuChina The Third People's Hospital of Bengbu Affiliated to Bengbu Medical University Department of Burn and Plastic SurgeryBengbu 230000AnhuiChina

Objective Our previous studies established that microRNA(miR)-451 from human umbilical cord mesenchymal stem cell-derived exosomes(hUC-MSC-Exos)alleviates acute lung injury(ALI).This study aims to elucidate the mechanisms by which miR-451 in hUC-MSC-Exos reduces ALI by modulating macrophage *** Exosomes were isolated from *** burn-induced ALI rat models were treated with hUC-MSC-Exos carrying the miR-451 ***-eosin staining evaluated inflammatory ***-linked immunosorbnent assay measured lipopolysaccharide(LPS),tumor necrosis factor-α,and interleukin-1β***-PCR detected miR-451 and tuberous sclerosis complex 1(TSC1)*** regulatory role of miR-451 on TSC1 was determined using a dual-luciferase reporter *** blotting determined TSC1 and proteins related to the mammalian target of rapamycin(mTOR)pathway and *** analysis was conducted to examine exosomes phagocytosis in alveolar macrophages and autophagy *** hUC-MSC-Exos with miR-451 inhibitor reduced burn-induced ALI and promoted macrophage ***-451 could be transferred from hUC-MSCs to alveolar macrophages via exosomes and directly targeted *** miR-451 in hUC-MSC-Exos elevated TSC1 expression and inactivated the mTOR pathway in alveolar *** TSC1 activated mTOR signaling and inhibited autophagy,while TSC1 knockdown reversed the autophagy from the miR-451 *** miR-451 from hUC-MSC exosomes improves ALI by suppressing alveolar macrophage autophagy through modulation of the TSC1/mTOR pathway,providing a potential therapeutic strategy for ALI.

关键词： Acute lung injury Human umbilical cord mesenchymal stem cell-derived exosomes MicroRNA-451 Tuberous sclerosis complex 1 Mammalian target of rapamycin pathway Autophagy

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In situ polymerization of water-induced 1,3-phenylene diisocyanate for enhanced efficiency and stability of inverted perovskite solar cells

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Interdisciplinary Materials 2024年第2期3卷 316-325页

作者： Shiyao Jia Jiabao Yang Tong Wang Xingyu Pu Hui Chen Xilai He guangpeng Feng Xingyuan Chen Yijun Bai Qi Cao Xuanhua Li State Key Laboratory of Solidification Processing Center for Nano Energy MaterialsSchool of Materials Science and EngineeringNorthwestern Polytechnical UniversityXi'anChina

In the realm of photovoltaics,organometallic hybridized perovskite solar cells(PSCs)stand out as promising contenders for achieving high-efficiency photoelectric conversion,owing to their remarkable performance ***,defects within the perovskite layer,especially at the perovskite grain boundaries and surface,have a substantial impact on both the overall photoelectric performance and long-term operational stability of *** mitigate this challenge,we propose a method for water-induced condensation polymerization of small molecules involving the incorporation of 1,3-phenylene diisocyanate(1,3-PDI)into the perovskite film using an antisolvent *** to this step,the introduction of water triggers the polymerization of[P(1,3-PDI)],thereby facilitating the in situ passivation of uncoordinated lead defects inherent in the perovskite *** passivation process demonstrates a notable enhancement in both the efficiency and stability of *** approach has led to the attainment of a noteworthy power conversion efficiency(PCE)of 24.66% in inverted ***,based on the P(1,3-PDI)modification,these devices maintain 90.15% of their initial efficiency after 5000 h of storage under ambient conditions of 25℃ and 50±5% relative ***,even after maximum power point tracking for 1000 h,the PSCs modified with P(1,3-PDI)sustain 82.05% of the initial *** molecules can rationally manipulate water and turn harm into benefit,providing new directions and methods for improving the efficiency and stability of PSCs.

关键词： antisolvent engineering defect passivation inverted perovskite solar cells

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大党独有难题的内在逻辑、生成动因与破解路径

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经济社会体制比较 2024年第3期 1-9页

作者：段光鹏山东大学马克思主义学院

大党独有难题作为具有大担当大胸怀大视野的政党提出的深刻问题,其中蕴含着鲜明的内在特征和丰富的基本意涵,需要通过科学研判“时”与“势”、理性辨别“大”与“小”、全面识别“干”与“枝”、正确比较“内”与“外”、辩证把握“危... 详细信息

大党独有难题作为具有大担当大胸怀大视野的政党提出的深刻问题,其中蕴含着鲜明的内在特征和丰富的基本意涵,需要通过科学研判“时”与“势”、理性辨别“大”与“小”、全面识别“干”与“枝”、正确比较“内”与“外”、辩证把握“危”与“机”,从中透视中国共产党居安思危的忧患意识、高瞻远瞩的眼界格局和未雨绸缪的政治自觉。大党独有难题的生成不是随机无序、凭空产生的,而是在使命意识的淡化、调适变革的滞后、讳疾忌医的态度、制度笼子的松动等互为因果、交相融合、相互助推的多种因素综合作用之下层积累迭的。破解大党独有难题是一项复杂的系统工程,需要绷紧政治建设之弦、把稳思想引领之舵、夯实长期执政之基、扎牢激浊扬清之笼、明确系统施治之策,以大党独有优势增强破解难题的整体效能,确保我们党始终走在时代前列。

关键词：大党独有难题自我革命全面从严治党

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面向元宇宙:数字时代共同富裕的发展新样态

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人文杂志 2024年第6期 119-129页

作者：段光鹏山东大学马克思主义学院

元宇宙作为数字虚拟世界和物理现实世界深度融合交互的重要平台,正在深刻形塑着共同富裕的发展样态和实施条件。借助虚拟现实技术、脑机交互技术、去中心化技术和数字孪生技术,元宇宙在共同富裕中构造分身的多元场景参与、延展感官的交... 详细信息

元宇宙作为数字虚拟世界和物理现实世界深度融合交互的重要平台,正在深刻形塑着共同富裕的发展样态和实施条件。借助虚拟现实技术、脑机交互技术、去中心化技术和数字孪生技术,元宇宙在共同富裕中构造分身的多元场景参与、延展感官的交互系统联动、统一身份认证的系统架构和打造环境的身临其境映射。面对元宇宙网络结构的分布化与技术运用的失衡化导致社会的不平等、用户活动的自由化与资本经营的垄断化导致平台的排他性、外部形式的共享化与内部形式的剥削化导致劳动的非正义、信息资源的集中化与规训行径的霸权化导致话语权被垄断等多重挑战,要从技术迭代升级、群体创造开放、治理边界拓展、立体叙事优化方面着力,通过共享元宇宙智慧实现共同富裕的新型样态。

关键词：元宇宙数字赋能共同富裕社会主义制度

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Key progresses of MOE key laboratory of macromolecular synthesis and functionalization in 2022

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Chinese Chemical Letters 2024年第3期35卷 114-126页

作者： Xumeng Deng Kaihao Chen Kai Pang Xiaoting Liu Minsong Gao Jie Ren Guanwen Yang guangpeng Wu Chengjian Zhang Xufeng Ni Peng Zhang Jian Ji Jianzhao Liu Zhengwei Mao Ziliang Wu Zhen Xu Haoke Zhang Hanying Li MOE Key Laboratory of Macromolecular Synthesis and Functionalization International Research Center for X PolymersDepartment of Polymer Science and EngineeringZhejiang UniversityHangzhou 310027China

In 2022,The MOE Key Laboratory of Macromolecular Synthesis and Functionalization in Zhejiang University had achieved several important ***,a series of well-defined dinuclear organoboron catalysts were developed to precisely control the enchainment of ether and carbonate segments during the copolymerization of CO_(2)and ***,polyester had been synthesized through cationic copolymerization of cyclic ***,ring-opening polymerization of carbon dioxide based valerolactone had been achieved,revealing the prospect of 3-ethylidene-6-vinyltetrahydro-2H-pyran-2-one(EVL)in utilizing CO_(2)and synthesizing functional ***,machine learning methods have been applied to biomaterial research,enabling high-throughput screening of functional biomaterial surfaces for implantable devices,and searching for potent antimicrobial peptides in whole combinatorial peptide ***,methods of characterization of biomacromolecule RNA transcription and manipulation of nucleoside modification were ***,artificial enzymes-armed Bifidobacterium Longum probiotics were established to tune down gut ***,three-dimensional(3D)printing technologies were used to engineer tough supramolecular ***,hydroplastic foaming graphene frameworks for acoustic and conductive polymer composites were provided for ***,aggregate photophysics about the nature of through-space interactions(TSIs)and manipulating their strength in small molecules with non-conjugated structure had been ***,the forming mechanism of a newfound nested texture in poly(L-lactic acid)(PLLA)spherulitic films had been ***,the isotropically dyeing mechanism of KDP single crystals grown from hydrogels have been *** related works are reviewed in this paper.

关键词： Polymer Catalyst Biomaterial research mRNA Hydrogel Graphene Crystal

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政党主导型现代化国家建设:中国式现代化的“新叙事”

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学习与实践 2024年第3期 13-23页

作者：段光鹏山东大学马克思主义学院山东济南250100

中国式现代化的理论体系与历史脉络呈现出政党主导的特征,全面建设社会主义现代化国家关键在党。中国的政党主导型现代化国家建设话语叙事,旨在塑造中国式现代化理论体系根本属性与正确认知的合理阐释,实现中国式现代化实践经验总结提... 详细信息

中国式现代化的理论体系与历史脉络呈现出政党主导的特征,全面建设社会主义现代化国家关键在党。中国的政党主导型现代化国家建设话语叙事,旨在塑造中国式现代化理论体系根本属性与正确认知的合理阐释,实现中国式现代化实践经验总结提升与实践引领的有效认同,进行中国式现代化他者论调事实澄明与独特模式的叙事引导。叙述好这一重大命题,要在一般与特殊的比较中论证“现代化”的探索历程,在自主与自觉的意识中把握“现代化”的主体力量,在使命与责任的实践中进行“现代化”的体制创新,在本土与世界的指向中展现“现代化”的价值指引。政党主导型现代化国家建设话语叙事具有丰富的延展空间和旺盛的生机活力,要在坚守话语导向、进行话语整合、提升话语阐释、打造话语标识等方面着力,不断创造创新出独具中国特色的现代化话语叙事体系。

关键词：中国共产党政党主导中国式现代化话语叙事

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基于细胞膜损伤机制的抗菌肽结构优化研究进展

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中国抗生素杂志 2023年第7期48卷 721-727页

作者：张良潘滢浩袁瑜黄波孟广鹏李元波周琳成都市药品检验研究院成都610045 成都诺和晟泰生物科技有限公司成都610000 成都中医药大学药学院成都610000

抗菌肽相比传统抗生素,具有广谱杀菌、对多重耐药菌有效、生物相容性好等优点。近年来,抗菌肽独特的细胞膜靶向作用机制得到了深入研究,基于此机制上的结构优化策略也成为了近期研究热点。本文主要针对抗菌肽的细胞膜损伤机制展开,就近... 详细信息

抗菌肽相比传统抗生素,具有广谱杀菌、对多重耐药菌有效、生物相容性好等优点。近年来,抗菌肽独特的细胞膜靶向作用机制得到了深入研究,基于此机制上的结构优化策略也成为了近期研究热点。本文主要针对抗菌肽的细胞膜损伤机制展开,就近期通过氨基酸替换、线性肽成环、化学修饰、多聚化、抗生素偶联以及复合材料制备等手段对抗菌肽结构予以优化的研究进展进行了总结,期望对抗菌肽设计与改构研究提供思路。

关键词：抗菌肽临床前研究结构优化

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