(2-萘氧基)乙酸甲酯置于lithium Hydroxide体系中,用 四氢呋喃,水 用作溶剂,化学反应生成2-萘氧乙酸 参考文献:Synthesis And Biochemical Evaluation Of Noncyclic Nucleotide Exchange Proteins Directly Activated By Camp 1 (Epac1) Regulators 标题:Synthesis And Biochemical Evaluation Of Noncyclic Nucleotide Exchange Proteins Directly Activated By Camp 1 (Epac1) Regulators 摘要:Exchange Proteins Directly Activated By Camp (Epac) Play A Central Role In Various Biological Functions,And Activation Of The Epac1 Protein Has Shown Potential Benefits For The Treatment Of Various Human Diseases. Herein,We Report The Synthesis And Biochemical Evaluation Of A Series Of Noncyclic Nucleotide Epac1 Activators. Several Potent Epac1 Binders Were Identified Including 25G,25Q,25N,25U,25E,And 25F,Which Promote Epac1 Guanine Nucleotide Exchange Factor Activity In Vitro. These Agonists Can Also Activate Epac1 Protein In Cells,Where They Exhibit Excellent Selectivity Toward Epac Over Protein Kinase A And G Protein-Coupled Receptors. Moreover,25E,25F,25N,And 25U Exhibited Improved Selectivity Toward Activation Of Epac1 Over Epac2 In Cells. Of These,25U Was Found To Robustly Inhibit Il-6-Activated Signal Transducer And Activator Of Transcription 3 (Stat3) And Subsequent Induction Of The Pro-Inflammatory Vascular Cell Adhesion Molecule 1 (Vcam1) Cell-Adhesion Protein. These Novel Epac1 Activators May Therefore Act As Useful Pharmacological Tools For Elucidation Of Epac Function And Promising Drug Leads For The Treatment Of Relevant Human Diseases. Doi:10.1021/acs.Jmedchem.9B02094
专利号:US-6451543-B1 优先权日:1998-08-31 标题:Lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides 发明人:KOCHENDOERFER GERD G; HUNTER CHRISTIE L; KENT STEPHEN B H; BOTTI PAOLO 权利人:GRYPHON SCIENCES 摘要:The present invention relates to methods and compositions for lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides that are incorporated in a lipid matrix. The invention is exemplified in production of a prefolded membrane polypeptide embedded within a lipid matrix via stepwise chemoselective chemical ligation of unprotected peptide segments, where at least one peptide segment is embedded in a lipid matrix. Any chemoselective reaction chemistry amenable for ligation of unprotected peptide segments can be employed. Suitable lipid matrices include liposomes, micelles, cell membrane patches and optically isotropic cubic lipidic phase matrices. Prefolded synthetic and semi-synthetic membrane polypeptides synthesized according to the methods and compositions of the invention also permit site-specific incorporation of one or more detectable moieties, such as a chromophore, which can be conveniently introduced during synthesis. The methods and compositions of the invention have multiple uses. For example, they can be used to assay ligand binding to membrane polypeptides and domains comprising a receptor, and thus are extremely useful for structure/function studies, drug screening/selection/design, and diagnostics and the like, including high-throughput applications. The methods and compositions of the invention are particularly suited for FRET analyses of previously inaccessible membrane polypeptides.
专利号:US-6264962-B1 优先权日:1997-12-19 标 题:Use of cinnamic acid or of at least one of its derivatives in a cosmetic composition 发明人:BRETON LIONEL; GIRERD FLORENCE; RENAULT BEATRICE 权利人:OREAL 摘要:The invention relates to the use of cinnamic acid, or of at least one of its derivatives, in a cosmetic composition as an agent for promoting the synthesis of the skin's total lipids. n The invention also relates to a cosmetic composition comprising an effective amount of cinnamic acid or of at least one of its derivatives.
专利号:US-4215044-A 优先权日:1979-04-23 标题:Synthesis of α-fluorocarbonyl compounds 发明人:MIDDLETON WILLIAM J 权利人:DU PONT 摘要:Process for preparing an organic compound of the formula R 2 R 2 CFC(O)R 3 , which process comprises contacting and reacting in a reaction mixture which includes an inert solvent, at a temperature of -40° C. to -100° C., ROF and ##STR1## R is polyfluoroperhaloalkyl of 1-6 carbon atoms or FOCF 2 ; R 1 is hydrocarbyl of 1-6 carbon atoms; n each R 2 is selected from H, alkyl of 1-17 carbon atoms, cycloalkyl of 3-6 carbon atoms, aryl, heteroaryl and such alkyl, cycloalkyl, aryl and heteroaryl substituted by halogen or alkoxy of 1-6 carbon atoms; n R 3 is selected from H, alkyl and haloalkyl of 1-16 carbon atoms, cycloalkyl of 3-10 carbon atoms, aryl and haloaryl, OSi(R 1 ) 3 , OH, NH 2 , alkoxy of 1-6 carbon atoms, aryloxy, NHR 1 and NR 1 2 wherein R 1 is alkyl of 1-6 carbon atoms, N-arylamino and nitrogen or sulfur heterocyclic of 4-5 carbon atoms; n R 3 and one R 2 taken together is a diradical which with the Câ•?C group is carbocyclic, heterocyclic or haloheterocyclic, and recovering from the reaction mixture the compound of the formula R 2 R 2 CFC()R 3 .
专利号:US-6660283-B2 优先权日:1997-12-19 标 题 :Use of cinnamic acid, or of at least one of its derivatives in a cosmetic composition 发明人:BRETON LIONEL; GIRERD FLORENCE; RENAULT BEATRICE 权利人:OREAL 摘要:The invention relates to the use of cinnamic acid, or of at least one of its derivatives, in a cosmetic composition as an agent for promoting the synthesis of the skin's total lipids.The invention also relates to a cosmetic composition comprising an effective amount of cinnamic acid or of at least one of its derivatives.
专利号:US-11149024-B2 优先权日:2017-03-31 标 题 :Synthesis of Mcl-1 inhibitor 发明人:STEWART CRAIG ROBERT; HARDY SIMON; STARK ANDREW; HIRD ALEXANDER; YE QING; ZHENG XIAOLAN; FERRAR CATI; KOEK JAN; HAZRA DEBASIS 权利人:ASTRAZENECA AB 摘要:Disclosed are intermediates and methods of synthesizing Compound 1.
专利号:US-2009047742-A1 优先权日:2005-08-24 标题 :Inhibition of mRNA Interferase-Induced Apoptosis in BAK-Deficient and BAK- and Bax-Deficient Mammalian Cells 发明人:SHIMAZU TSUTOMU; DEGENHARDT KURT; WHITE EILEEN; INOUYE MASAYORI 权利人:UNIV NEW JERSEY MED 摘要:Ribonucleases, antibiotics, bacterial toxins and viruses inhibit protein synthesis, which results in apoptosis in mammalian cells. How the BCL-2 family of proteins regulates apoptosis in response to shutoff of protein synthesis is not known. According to the present invention, an Escherichia coli toxin MazF inhibited protein synthesis by cleavage of cellular mRNA, and induced apoptosis in mammalian cells. MazF-induced apoptosis required proapoptotic BAK and its upstream regulator, the proapoptotic BH3-only protein NBK/BIK, but not BIM, PUMA or NOXA. Furthermore, NBK/BIK- or BAK-deficient cells were resistant to cell death induced by pharmacologic inhibition of translation and by virus-mediated shutoff of protein synthesis. Thus, the BH3-only protein NBK/BIK is the apical regulator of a BAK-dependent apoptotic pathway in response to shutoff of protein synthesis. Although NBK/BIK is dispensable for development, it is the BH3-only protein targeted for inactivation by viruses, suggesting that it plays a role in pathogen/toxin response through apoptosis activation.
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合成参考文献
参考文献:10.1093/jxb/ern133 摘要:Christian M, Hannah WB, Lüthen H, Jones AM. Identification of auxins by a chemical genomics approach. J Exp Bot. 2008;59(10):2757–67.