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Highly Diasteroselective Friedel-Crafts Reaction of Indoles with N-tert-Butanesulfinylimino Esters:An Efficient and Practical Approach to Enantiomerically Enriched Indolylglycines

Highly Diasteroselective Friedel-Crafts Reaction of Indoles ...

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13th Asian Chemical Congress

作者： Du-Ming JI and Ming-Hua XU~* shanghai institute of materia medica chinese academy of sciences 555 Zuchongzhi Road shanghai 2.12.3 china.

＜正＞Optically active non-proteinogenic amino acids are currently of great interest due to their significant biological activities,and extensive applications in new drug *** these valuable amino acids,indolylglycines that exist in many biologically natural and unnatural products have attracted much *** their asymmetric synthesis,however,despite the strategies of asymmetric catalysis,enzymatic resolution and chiral auxiliary-mediated induction were used;far

关键词： indolylglycine N-tert-butanesulfinyl imine Friedel-Crafts reaction

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Involvement of actin rearrangements within the amygdala and the dorsal hippocampus in aversive memories of drug withdrawal in acute morphine dependent rats

Involvement of actin rearrangements within the amygdala and ...

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中国神经科学学会第四次会员代表大会暨第八届全国学术会议

作者： Yuan-Yuan HOU,Bin LU,Mu LI,Yao LIU,Jie CHEN,Zhi-Qiang CHI,Jing-Gen LIU~* state key laboratory of drug research,shanghai institute of materia medica,chinese academy of sciences,shanghai 2.12.3,china

＜正＞Objective Aversive memories of drug withdrawal can generate a motivational state leading to compulsive drug *** in synaptic plasticity may be involved in the formation of aversive *** rearrangement of the cytoskeletal actin,a major structural component of the dendritic spine,regulates synaptic *** present study is to examine the potential involvement of actin rearrangements in the induction of aversive memories of morphine *** Conditioned place aversion（CPA） paradigm was used to examine the involvement of actin rearrangements in the induction of aversive memories of drug *** observe actin rearrangements in the synapse,the alteration of F-actin and G-actin content was examined by western blot *** of the amygdala,dorsal hippocampus （DH） and nucleus accumbens（NAc） were produced by local microinjection of ibotenic *** We found that lesions of the amygdala or DH,but not NAc,impaired conditioned place aversion of acute morphine dependent rats. Accordingly,conditioned morphine withdrawal induced actin rearrangements in the amygdala and the DH but not in the NAc,characterized by a net increase in F-actin content in the *** addition,we found that conditioned morphine withdrawal also increased activity-regulated cytoskeletal-associated protein（Arc） expression in the amygdala but not in the DH,although actin rearrangements were observed in both *** further found that inhibition of actin rearrangements by intra-amygdala or intra-DH injections of latrunculin A,an inhibitor of actin polymerization,significantly attenuate CPA ***,we found that the inhibition of amygdala P-adrenoceptor activity by its antagonist propranolol diminished actin rearrangement in the DH induced by conditioned morphine withdrawal while the stimulation of amygdalaβ-adrenoceptor activity by its agonist clenbuterol elicited actin rearrangements in the DH without morphine withdrawal ***

关键词： actin rearrangement withdrawal memory amygdale dorsal hippocampus morphine addiction

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Chronic morphine treatment impaired hippocampal long-term potentiation and spatial memory via accumulation of extracellular adenosine acting on adenosine Al receptors

Chronic morphine treatment impaired hippocampal long-term po...

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中国神经科学学会第九届全国学术会议暨第五次会员代表大会

作者： Gang LU~1,Qi-Xin ZHOU~2,Shuo KANG~1,Lin XU~2,Jing-Gen LIU~(1,*) 1 state key laboratory of drug research,shanghai institute of materia medica,shanghai institute For biological sciences,chinese academy of sciences,shanghai 2.12.3,china.2 key laboratory of Animal Models and Human Disease Mechanisms of chinese academy of sciences & Yunnan Province,Kunming institute of Zoology,Kunming 650223,china

＜正＞Chronic exposure to opiates impairs hippocampal long-term potentiation（LTP） and spatial memory, but the underlying mechanisms remain to be *** the well known effects of adenosine,an important neuromodulator,on hippocampal neuronal excitability and synaptic plasticity,we investigated the potential effect of changes in adenosine concentrations on chronic morphine treatment-induced impairment of hippocampal CA1 LTP and spatial *** found that chronic treatment in mice with either increasing doses（20-100 mg/kg） of morphine for 7 d or equal daily dose（20 mg/kg） of morphine for 12 d led to a significant increase of hippocampal extracellular adenosine ***,we found that accumulated adenosine contributed to the inhibition of the hippocampal CA1 LTP and impairment of spatial memory retrieval measured in the Morris water *** A1 receptor antagonist 8-cyclopenty1-1,3-dipropylxanthine significantly reversed chronic morphine-induced impairment of hippocampal CA1 LTP and spatial ***,adenosine deaminase,which converts adenosine into the inactive metabolite inosine,restored impaired hippocampal CA1 *** further found that adenosine accumulation was attributable to the alteration of adenosine uptake but not adenosine *** nucleoside transporters（ENT2） appeared to play a key role in the reduction of adenosine *** in PKC-α/βactivity were correlated with the attenuation of the ENT2 function in the short-term（2 h） but not in the long-term（7 d） period after the termination of morphine *** study reveals a potential mechanism by which chronic exposure to morphine leads to impairment of both hippocampal LTP and spatial memory.

关键词： morphine spatial memory adenosine PKC LTP ENT

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A Facile Synthesis of 3-Arylbenzothiophenes

A Facile Synthesis of 3-Arylbenzothiophenes

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中国化学会第四届有机化学学术会议

作者： YANG, Chun-Hao LIU, Bo XU, Guang-Yu XIE,Yu-Yuan (state key laboratory of drug research, shanghai institute of materia medica, chinese academy of Science, shanghai 2.12.3)

＜正＞Benzothiophene derivatives exhibit a variety of biological properties. Although there are general methods to synthesize 2-arylbenzothiophene, few methods are available for 3-arylbenzothiophene. These methods are usually not satisfactory due to toxic reagent or tedious workup procedure: catalyst should be activated over 300℃, the generated water should be removed from the reaction mixture and product isolation need expensive HPLC instrument.

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中国红树植物红海榄(Rhizophora stylosa)的化学成分研究

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天然产物研究与开发 2004年第1期16卷 23-25页

作者：赵亚宋国强郭跃伟中国科学院上海生命科学院上海药物研究所国家新药研究重点实验室上海201203

从红树科红海榄 (Rhizophorastylosa)小枝的石油醚提取物中分得 5个三萜化合物 ,通过波谱方法鉴定 ,它们分别是taraxerol (1) ,taraxerone (2 ) ,careaborin (3) ,cis careaborin (4 )和 palmitoyl β amyrin(5 ) ,均为首次从该植物中... 详细信息

从红树科红海榄 (Rhizophorastylosa)小枝的石油醚提取物中分得 5个三萜化合物 ,通过波谱方法鉴定 ,它们分别是taraxerol (1) ,taraxerone (2 ) ,careaborin (3) ,cis careaborin (4 )和 palmitoyl β amyrin(5 ) ,均为首次从该植物中分得。

关键词：中国红树科红海榄药材三萜植物化学成分

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维普期刊数据库

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长叶水麻化学成分的研究

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天然产物研究与开发 2003年第1期15卷 21-23页

作者：秦波汪汉卿朱大元中国科学院上海生命科学研究院上海药物研究所新药研究国家重点实验室上海200031 中国科学院兰州化学物理研究所OSSO国家重点实验室兰州730000

长叶水麻 (Debregeasialongifolia(Burm .f.)Wedd .)是荨麻科植物 ,果可食 ;根入药 ,除风湿。本文首次从其枝、叶乙醇提取物的乙酸乙酯萃取部位分离鉴定出 5种黄酮甙类化合物 ,它们分别是 :epicat echin(化合物 1) ,quercetin 3 O β D ... 详细信息

长叶水麻 (Debregeasialongifolia(Burm .f.)Wedd .)是荨麻科植物 ,果可食 ;根入药 ,除风湿。本文首次从其枝、叶乙醇提取物的乙酸乙酯萃取部位分离鉴定出 5种黄酮甙类化合物 ,它们分别是 :epicat echin(化合物 1) ,quercetin 3 O β D galactopyranoside(化合物 2 ) ,kaempferol 3 O β D galactopyranoside(化合物 3) ,quercetin 7 O β D glucopyranoside(化合物 4 ) ,apigenin 7 O β D glucopyranoside(化合物 5 )。

关键词：长叶水麻化学成分黄酮黄酮甙荨麻科

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维普期刊数据库

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SPR technology and CD spectra in interaction between PPARγ-LBD and LigandsSPR technology and CD spectra in interaction between PPARγ-LBD and Ligands

SPR technology and CD spectra in interaction between PPARγ-...

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华东六省一市生物化学与分子生物学会2003年学术交流会

作者： Chang-ying Yu, Lili Chen, Feng Cheng, Rui-hao Zhang, Jian-hua Shen, Hua-liang Jiang, Xu Shen ( drug Discovery and Design Center, state key laboratory of drug research, shanghai institute of materia medica, shanghai institutes for biological sciences, chinese academy of sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, shanghai 2.12.3, china.

PPAHγis a ligand-dependent transcription factor. It plays an important role in the regulation of adipocytefunction and systemic lipid homeostasis. PPARγparticipates in the biological pathways of basic and clinical inter-est,such as insulin sensitivity, type 2 diabetes and therosclerosis. In this report, the ligand binding characteristicsof a series of commercially available PPARγligands (GW9662, GI 262570, CPA, 15-d-PGJ, LY171883, Indom-ethacin, Linoleic acid, Palmitic acid and Troglitazone) to human PPARγligand-binding domain (LBD) were in-vestigated hy surface plasmon resonance biosensor (SPR) technology BIAcore 3000 and circular dichroism (CD)

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Discovery of potent and selective c-Met inhibitor

Discovery of potent and selective c-Met inhibitor

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2011年全国药物化学学术会议——药物的源头创新

作者： Fang Chen,~aJing Ai,~b Ying Wang,~b Zhengsheng Zhan,~a Yongcong Lu,~a Yi Chen,~b Jian ding,Meiyu Geng~b and Wenhu Duan~(*,a) a Department of Medicinal Chemistry,shanghai institute of materia medica,chinese academy of sciences,shanghai 2.12.3,PR china.bDivision of Anti-tumor Pharmacology,state key laboratory of drug research,shanghai institute of materia medica,chinese academy of sciences,shanghai 2.12.3,PR china

＜正＞HGF/c-Met signaling pathway mediates a variety of important biological activities but deregulation of the pathway is closely associated with poor prognosis in a number of major human ***,c-Met has been considered as a good target for anti-cancer drug ***,we report the discovery of a series of triazolotriazine derivatives as selective

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Structural Basis for Ubiquitin Recognition by a Novel Domain from Human Phospholipase A2 Activating Protein

Structural Basis for Ubiquitin Recognition by a Novel Domain...

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第十一次中国生物物理学术大会暨第九届全国会员代表大会

作者： Qing-Shan Fu ,Chen-Jie Zhou ,Hong-Chang Gao ,Ya-Jun Jiang ,Zi-Ren Zhou ,Jing Hong ,Wen-Ming Yao ,Ai-Xin Song ,Dong-Hai Lin 1 ,and Hong-Yu Hu 1 state key laboratory of Molecular Biology,institute of Biochemistry and Cell Biology,shanghai institutes for biological sciences,chinese academy of sciences, shanghai 200031 china.shanghai institute of materia medica,shanghai institutes for biological sciences, chinese academy of sciences,shanghai 2.12.3,china.$Graduate School of the chinese academy of sciences,19A Yu Quan Road,Beijing 100039,china

＜正＞Ubiquitin（Ub）is an essential modifier conserved in all eukaryotes from yeast to *** A2 activating protein（PLAA）,a mammalian homolog of yeast DOA1/UFD3,

关键词： ubiquitin ubiquitin-binding domain solution structure cis/trans isomerization PLAA.

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Activation of PI-Linked Dl-Like receptor modulates FGF-2 expression in astrocytes via IP3-dependent Ca2+ signaling

Activation of PI-Linked Dl-Like receptor modulates FGF-2 exp...

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中国神经科学学会第四次会员代表大会暨第八届全国学术会议

作者： Xin-Hua ZHANG~(1,2,4),Zheng ZHOU~2,Da-Kui WANG~(2,3),Ai-Qun LI~1,Yan-Qing YIN~2,Xiao-Song GU~3,Fei DING~3,Xue-Chu ZHEN~(5,*),Jia-Wei ZHOU~(2,*) 1 laboratory of Molecular Cell Biology,institute of Biochemistry and Cell Biology 2 institute of Neuroscience,state key laboratory of Neuroscience,shanghai institutes for biological sciences,chinese academy of sciences,shanghai,200031,china.3 Jiangsu key laboratory of Neuroregeneration,Nantong University School of Medicine,Nantong,226001,china.4 Department of Anatomy,Nantong University School of Medicine,Nantong,226001,china.5 state key laboratory of drug research,shanghai institute of materia medica,shanghai institutes for biological sciences,chinese academy of sciences,shanghai,2.12.3,china

FGF-2 is predominantly synthesized and secreted by astrocytes in adult *** previous study showed that activation of classical dopamine receptor D1 or D2 elicits FGF-2 biosynthesis and secretion in ***,we report that astrocytic FGF-2 expression is also regulated by phosphatidylinositol(PI)-linked D1-like ***83959,a selective Pi-linked D1-like receptor agonist,upregulates the levels of FGF-2 protein in striatal astrocyte cultures in classical dopamine D1 and D2 receptor-independent *** conditional medium derived from SKF83959-activated astrocytes promoted the number of TH+ neurons in *** of astrocytes with SKF83959 increased intracellular calcium in two *** of intracellular calcium oscillation by inositol 1,4,5-triphosphate(TP3) inhibitors blocked the SKF83959-induced increase in FGF-2 ***,intraperitoneal administration of SKF83959 reversed MPTP-induced reduction in FGF-2 expression in both the striatum and ventral midbrain and resulted in marked protection of dopaminergic neurons from MPTP-induced *** results indicate that IP3/Ca/calmodulin-dependent protein kinase(CaMK) is an uncharted intracellular signaling pathway that is crucial for the regulation of FGF-2 synthesis in ***-linked Dl-like receptor plays an important role in the regulation of astrocytic FGF-2 expression and neuroprotection which may provide a potential target for the drug discovery in Parkinson’s disease.

关键词： striatum neurotrophic factor Parkinson’s disease signal transduction astrocyte FGF-2

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