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Asymmetric Synthesis of (-)-(4R, 5R)-4-[5-(Benzo[1, 3]dioxol-5-yl)-4- hydroxyl-1-(pyridin-2-yl)-4, 5-dihydro-1H-pyrazol-3-yl]benzamide

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Chinese Chemical Letters 2005年第9期16卷 1137-1139页

作者： Xing Zhou LI Xian Ping DAI jun hai xiao Song LI Beijing Institute of Pharmacology ＆ Toxicology Beijing 100850 School of pharmaceutical Engineering Shenyang Pharmaceutical University Shengyang 110016

The asymmetric synthesis of （-）-（4R, 5R）-4-[5-（benzo[1, 3]dioxol-5-yl）-4-hydroxyl-1- （pyridin-2-yl）-4,5-dihydro-lH-pyrazol-3-yl]-benzamide with improved Juliá-Colonna asymmetric epoxidation procedure as key s... 详细信息

关键词： Asymmetric synthesis Juliá-Colonna epoxidation 1,3,5-triaryl-4-hydroxyl-4,5-dihydro-1H-pyrazole

Design,synthesis,and screen of cathepsin K inhibitors

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Chinese Chemical Letters 2013年第8期24卷 715-718页

作者： Ying-Ying Yu Wei Sun Lei Dong hai-Dong Liu Dan Jiang jun-hai xiao xiao-Hong Yang Song Li School of Pharmaceutical Sciences Jilin University Laboratory of Computer-Aided Drug Design and Discovery Beijing Institute of Pharmacology and Toxicology First Affiliated Hospital of Jilin University

We synthesized a series of epoxysuccinic acid derivatives and evaluated their in vitro cathepsin K inhibitory activity The screening results show that the potency of compounds 9e,9d,9p,9j and 9k （IC_（50）≤0.005μmol/L） were equal to or greater than that of the lead compound *** hydrophobic compounds showed weaker potency,which can be explained by the hydrophobic nature of the cathepsin K binding pockets.

关键词： Epoxysuccinic acid derivatives Synthesis Inhibitors Cathepsin K

Molecular characterization of three Hsp90 from Pieris and expression patterns in response to cold and thermal stress in summer and winter diapause of Pieris melete

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Insect Science 2018年第2期25卷 273-283页

作者： Yue-Kun Wu Chao Zou Dao-Meng Fu Wan-Na Zhang hai-jun xiao Institute of Entomology Jiangxi Agricultural University Nanchang China Institute of Plant Protection Chinese Academy of Agricultural Sciences Beijing China

Heat shock proteins （Hsps） have been linked to stresses and winter diapause in insects, but whether they are components of summer diapause is still unknown. In this study, complementary DNAs of lisp90 from Pieris melete, Pieris rapae and Pieris canidia named PmHsp90, PrHsp90 and PcHsp90, respectively, were cloned and sequenced. The deduced amino acid sequence consisted of 718 amino acid residues with a putative molecular mass of 82.6, 82.6 and 82.7 kDa, respectively. The amino acid sequences contained all of the five conserved signature motifs in the Hsp90 family and a bHLH protein folding activity region. The differential expression pattern of PmHsp90 in response to summer diapause and winter diapause, which are related to heat/cold stress, was investigated. Cold stress induced Hsp90 up-regulation in summer and winter diapause pupae, but not in non-diapause individuals. Heat shock up-regulated PmHsp90 gradually with an increase in temperature in summer diapause, and PmHsp90 was rapidly up-regulated in winter diapause. After 30 min heat shock at 39℃, substantial up-regulation of PmHsp90 transcript levels were observed both in summer and winter diapause. However, in non-diapause a relatively stable expression was found under different durations of 39℃ heat shock. Compared to the optimal treatment of 18℃ for diapause development, a high temperature acclimation of 31 ℃ induced PmHsp90 up-regulation in summer diapause, whereas a low temperature acclimation of 4℃ induced up-regulation in winter diapause. The current results indicate that Hsp90 may play an important role in response to heat/cold stress both in summer and winter diapause.

关键词： Hsp90 Pieris melete Pieris rapae Pieris canidia summer and winterdiapause cold and heat shock

Synthesis of 5-substituted benzyl-2,4-diamino pyrimidine derivatives as c-Fms kinase inhibitors

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Chinese Chemical Letters 2010年第11期21卷 1318-1321页

作者： Li Bao Xu Wei Sun Hong Ying Liu Li Li Wang jun hai xiao xiao Hong Yang Song Li School of Pharmaceutical Sciences Jilin University Changchun 130021 China Laboratory of Computer-Aided Drug Design & Discovery Beijing Institute of Pharmacology and Toxicology Beijing 100850 China

A serials of novel 5-substituted benzyl-2,4-diamino pyrimidine derivatives have been synthesized and evaluated as inhibitors of c-Fms kinase by the standard MTT *** results showed that compound 15,5-[3-methoxy-4-（pyridine-3-yl）benzyl]-2,4-diamino pyrimidine,had an IC50 of 1.45μmol/L in inhibiting the proliferation of M-CSF-dependent myeloid leukemia cells in mice （NFS-60）,which was similar with GW2580,a selective inhibitor of c-Fms kinase.

关键词： C-Fms kinase inhibitors Synthesis 2 4-Diamino pyrimidine

Synthesis of benzocycloheptene derivatives as CCR5 antagonists with potent anti-HIV activity

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Chinese Chemical Letters 2008年第4期19卷 428-430页

作者： Yao Liu Jing Su jun hai xiao Shi Bo Jiang Hong Lu Wu Zhong Li Li Wang xiao Hong Yang Song Li School of Pharmacy Jilin UniversityChangchun 130021China School of Pharmacy Shanghai Jiaotong UniversityShanghai 200240China Institute of Pharmacology and Toxicology Academy of Military Medical SciencesBeijing 100850China Lindsley E Kimball Research Institute The New York Blood CenterNew YorkNY 10021USA

A series of novel benzocycloheptene derivatives have been *** structures were confirmed by MS and ^1H-NMR. These compounds exhibited potent anti-HIV-1 activities.

关键词： HIV-1 entry inhibitors Benzocycloheptene derivatives Synthesis

Screening of chemokine receptor CCR4 antagonists by capillary zone electrophoresis

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Journal of Pharmaceutical Analysis 2011年第4期1卷 264-269页

作者： Zhe Sun Lin-Jie Tian Qian Lin xiao-Mei Ling jun-hai xiao Ying Wang Department of Pharmaceutical Analysis of School of Pharmaceutical Sciences and State Key Laboratory of Natural andBiomimetic DrugsPeking UniversityBeijing 100191PR China Center for Human Disease Genomics and Department of Medical Immunology of School of Basic Medical SciencePeking UniversityBeijing 100191PR China Beijing Institute of Pharmacology and Toxicology Beijing 100850PR China

CC chemokine receptor 4(CCR4)is a kind of G-protein-coupled receptor,which plays a pivotal role in allergic *** interaction between 2-(2-(4-chloro-phenyl)-5-{[(naphthalen-1-ylmethyl)-carbamlyl]-methyl-4-oxo-thiazolidin-3-yl)-N-(3-morpholin-4-yl-propyi)-acetamide(S009)and the N-terminal extracellular tail(ML40)of CCR4 has been validated to be high affinity by capillary zone electrophoresis(CZE).The S009 is a known CCR4 ***,a series of new thiourea derivatives have been *** with positive control S009,they were screened using ML40 as target by CZE to find some new drugs for allergic inflammation *** synthesized compounds XJH-5,XJH-4,XJH-17 and XJH-1 displayed the interaction with ML40,but XJH-9,XJH-10,XJH-I 1,XJH-12,XJH-13,XJH-14,XJH-3,XJH-8,XJH-6,XJH-7,XJH-15,XJH-16 and XJH-2 did not bind to *** qualification and quantification characterizations of the binding were *** affinity of the four compounds was valued by the binding constant,which was similar with the results of chemotactic *** established CEZ method is capable of sensitive and fast screening for a series of lactam analogs in the drug discovery for allergic inflammation diseases.

关键词： Capillary zone electrophoresis CCR4 antagonist 2-(2-(4-chloro-phenyl)-5-{[(naphthalen-1-ylmethyl)-carbamoyl]-methyl}-4-oxo-thiazoli-din-3-yl)-N-(3-morpho-lin-4-yl-propyl)-aceta-mide Interactions Structural modification

Synthesis of 1-aryl-3-(3,4-dihydro-2H-chromen-5-yl) ureas as TNF-αinhibitors

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Chinese Chemical Letters 2007年第8期18卷 905-908页

作者： Xin Ming Zhou Zhi Bing Zheng Hong Ying Liu Wu Zhong jun hai xiao Li Li Wang Song Li Institute of Pharmacology and Toxicology Academy of Military Medical Sciences Beijing 100850 China School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 China

A new series of compounds, 1-aryl-3-（3,4-dihydro-2H-chromen-5-yl） ureas, have been synthesized and their structures were confirmed by FAB-MS and IH NMR. The preliminary pharmacological screening showed that these co... 详细信息

关键词： p38 MAPK inhibitor l-Aryl-3-(3,4-dihydro-2H-chromen-5-yl) ureas Synthesis

Catalyst-free and Reprocessable Aromatic Polydithiourethanes

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Chinese Journal of Polymer Science 2024年第10期42卷 1435-1441,I0007页

作者： Bo Yang hai-jun Feng Tian-Tian Ni xiao-Rui Zhou Tao Xie Ning Zheng State Key Laboratory of Chemical Engineering College of Chemical and Biological EngineeringZhejiang UniversityHangzhou310058China Department of Colorectal Surgery and Oncology Key Laboratory of Cancer Prevention and InterventionMinistry of EducationThe Second Affiliated HospitalZhejiang University School of MedicineHangzhou310009China

The incorporation of dynamic covalent bonds into thermosets facilitates the reprocessing of polymer networks,thereby meeting the sustainable requirements for polymer ***,the mechanical properties of many materials often decline significantly upon reprocessing due to side reactions caused by harsh processing *** this work,we find that the aromatic dithiocarbamate bond can undergo dissociation under mild conditions without the need for a catalyst,enabling the efficient reprocessing of the corresponding *** a consequence,the mechanical properties of the polydithiourethane can be largely preserved after *** discovery of this dynamic chemistry is anticipated to broaden the potential for material design in dynamic covalent polymer networks.

关键词： Reprocessing Polydithiourethane Dynamic covalent bond

A rare case of isolated non-compaction right ventricular myocardium

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Chinese Medical Journal 2009年第14期122卷 1718-1720页

作者： ZHANG xiao-juan ZHI Guang HOU hai-jun ZHOU xiao Cardiology Ward. Chinese PLA General Hospital. Beijing 100853 China

Isolated right ventricular noncompaction （IRNC） is a rare congenital cardiomyopathy resulting from an arrest in normal endomyocardial embryogenesis. The clinical syndrome includes systolic and diastolic dysfunction： some cases may have ventricular arrhythmias. We report a case of a female with the diagnosis of right ventricular non-compaction myocardium （RVNC） with normal left ventricular systolic function. To the best of our knowledge, there have been no reports of isolated ventricular non-compaction involving only the right ventricular before 2008. and there have only been described in very few cases of newborns and adult patients.

关键词： cardiomyopathies heart failure: echocardiography