(3-(benzofuran-3-yl)-4-indolin 2 one-3yl maleimides)

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2-Oxiranecarboxylicacid, 3-methyl-, 1-methylethyl ester, (2S,3R)-2-Oxiranecarboxylicacid, 3-methyl-, 1-methylethyl ester, (2R,3S)-rel-Methanone,[2-[2-(dimethylamino)-5-hydroxy-3-benzofuranyl]-5-methoxynaphtho[1,2-b]furan-3-yl]phenyl-5(4H)-Oxazolone,4-cyclopentyl-2-ethyl-Benzoic acid,4-(4-cyclopentyl-2-ethyl-4,5-dihydro-5-oxo-4-oxazolyl)-, methyl esterS-[3-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)propyl] ethanethioate3-溴-2,6-二氟甲苯2,4-Difluoro-3-methylbromobenzene3,6,9,12,15,18,21-Heptaoxadotriacontanoicacid, 32-mercapto-2-[(E)-2-(2-methylphenyl)ethenyl]-4,5-dihydro-1H-imidazole ethanedioate (1:1)L-Arginine,N-(1-oxohexadecyl)glycyl-L-glutaminyl-L-prolyl-4-(甲基磺酰氧甲基)-1,2-O-二乙酰氧基-3,5-O-二苄基-alpha-D-赤式戊呋喃糖4-(Methanesulfonyloxymethyl)-1,2-O-diacetoxy-3,5-O-dibenzyl-alpha-D-erythro-pentofuranose9(10H)-Acridinone,2-chloro-6-methyl-10-(phenylmethyl)-2H-1,2-Benzothiazine-3-carboxylic acid,4-(7-ethyl-1,3-benzodioxol-5-yl)-2-[2-(trifluoromethyl)phenyl]-,1,1-dioxideBenzenebutanoic acid, a-amino-4-hydroxy-, (aS)-5-amino-1-tert-butyl-3-naphthalen-2-yl-1H-pyrazole-4-carbonitrile1-tert-butyl-3-(naphthalen-1-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine1,4-bis{2-[2-(2-methoxyethoxy)ethoxy]ethoxy}benzene1-tert-butyl-3-(naphthalen-1-ylmethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine1,2-Benzenediol,5-bromo-3-ethyl-2-Cyclohexen-1-one,3-(hydroxymethyl)-6-(1-methylethylidene)-2-Cyclohexen-1-one,4-hydroxy-3-methyl-6-(1-methylethylidene)-5-Heptenoic acid,7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-[(1E,3S)-3-hydroxy-5-[3-(trifluoromethyl)phenyl]-1-penten-1-yl]cyclopentyl]-,(5Z)-6-Bromo-4-nitro-2,2'-bipyridine5-Methyl-4'-nitro-2,2':6',2''-terpyridine5,5''-Dimethyl-4'-nitro-2,2':6',2''-terpyridine5,5''-Dimethyl-2,2':6',2''-terpyridin-4'-amineCarbamic acid,[(1S)-1-(4-methoxyphenyl)ethyl]-, 1,1-dimethylethyl ester (9CI)Cyclopentanemethanol,2-(acetyloxy)-, 1-acetate, (1R,2R)-2-[methyl(7-nitro-2,1,3-benzoxadiazol-4-yl)amino]acetohydrazide (non-preferred name)Acetamide,N-[(3-chloro-1-methyl-1H-pyrazol-5-yl)methyl]-(2-amino-6-fluorophenyl)methanol[(3R,4R,5R,6R)-3,4,5-trihydroxy-6-[2-[(5-nitrothiazol-2-yl)carbamoyl]phenoxy]tetrahydropyran-2-carbonyl]oxysodiummethyl (3R,4R,5R,6R)-3,4,5-triacetoxy-6-(2-benzyloxycarbonylphenoxy)tetrahydropyran-2-carboxylate2-[(2R,3R,4R,5R)-3,4,5-triacetoxy-6-methoxycarbonyl-tetrahydropyran-2-yl]oxybenzoic acidmethyl (3R,4R,5R,6R)-3,4,5-triacetoxy-6-[2-[(5-nitrothiazol-2-yl)carbamoyl]phenoxy]tetrahydropyran-2-carboxylate1H-Benzimidazole-5-carbonitrile,2,3-dihydro-2-oxo-6-Quinoxalinecarbonitrile,1,2,3,4-tetrahydro-2-oxo-[3-(tert-butylsulfamoyl)phenyl]boronic acid1H-Benzimidazole-5-carbonitrile,2,3-dihydro-1-methyl-2-oxo-Propanamide,2-methyl-N-[(3S)-tetrahydro-2-oxo-3-furanyl]-5-bromopyrazine-2-carbonitrile2-Pyrazinecarbonitrile,5-(dimethylamino)-2-Pyrazinecarboxaldehyde,5-(dimethylamino)-Carbamic acid,[2-[(3-aminopropyl)amino]ethyl]-, 1,1-dimethylethyl ester (9CI)(3-methylpiperidin-3-yl)methanol4,4-二联环己酮 单(2,2-二甲基-)丙二缩酮4,4'-Bi(cyclohexanone) neopentyl glycol monoacetal1H-Pyrazole-4-carboxamide,3-methoxy-1H-Pyrazole-3-carboxylicacid, 4-fluoro-, ethyl ester1H-1,2,4-Triazol-1-amine,3-nitro-4-(2,6-dimethylphenoxy)benzene-1,2-dicarbonitrile2-Azetidinone,1-ethenyl-4-(2-propen-1-yloxy)-Benzene,1-fluoro-4-(3-methyl-1,2-butadien-1-yl)-Benzene,1-fluoro-4-(1-methyl-1,2-propadien-1-yl)-6-三氟甲基烟酸甲酯Methyl 6-(trifluoromethyl)nicotinate6-(trifluoromethyl)pyridine-3-carboximidamide hydrochloride1,4-Dioxaspiro[4.4]nonane-2-carboxaldehyde,3-methyl-, (2S,3R)-2-(2,2-dimethylpropanoyloxymethyl)thiazole-4-carboxylic acid2-(hydroxymethyl)-1,3-thiazole-4-carboxylic acid1H-Pyrazole-3-carboxylicacid, 5-formyl-1-methyl-1H-Pyrazole-5-carboxylicacid, 3-formyl-1-methyl-3H-Pyrazol-3-one,2,4-dihydro-4,4-dihydroxy-5-methyl-3H-Pyrazol-3-one,2-ethyl-2,4-dihydro-4,4-dihydroxy-5-methyl-3H-Pyrazol-3-one,2,4-dihydro-4,4-dihydroxy-5-methyl-2-(1-methylethyl)-3H-Pyrazol-3-one,2,4-dihydro-4,4-dihydroxy-5-methoxy-2-methyl-Acetamide,N-(4,5-dihydro-4,4-dihydroxy-1-methyl-5-oxo-1H-pyrazol-3-yl)-3H-Pyrazol-3-one,2,4-dihydro-4,4-dihydroxy-2-(1-methylethyl)-3H-Pyrazol-3-one,5-ethoxy-2,4-dihydro-4,4-dihydroxy-spiro[3.5]nonane-6,8-dionePhenol,5-isocyanato-2-methyl-5-氟苯并恶唑5-Fluorobenzoxazole2-methoxy-3-nitropyridine-4-carbaldehyde2-methoxy-4-(1-methoxyvinyl)-6-methyl-3-nitro-pyridine2-methoxy-6-methyl-3-nitropyridine-4-carbaldehydeN-叔丁氧羰基-D-烯丙基甘氨酸二环己胺盐Boc-D-Allylglycine dicyclohexylamine salt1-[1-(tert-butoxycarbonyl)piperidin-4-yl]-L-proline2-(tert-butoxycarbonyl)-2,3-dihydro-1H-isoindole-1-carboxylic acid(5R)-1-(tert-butoxycarbonyl)-5-phenyl-L-proline1,2-Pyrrolidinedicarboxylicacid, 4-[[(1,1-dimethylethoxy)carbonyl]amino]-, 1-(9H-fluoren-9-ylmethyl)ester, (2S,4S)-1-Piperidineaceticacid, 4-[[(9H-fluoren-9-ylmethoxy)carbonyl]amino]-9H-fluoren-9-ylmethyl piperidin-3-ylcarbamate hydrochloride9H-fluoren-9-ylmethyl [2-(2-aminoethoxy)ethyl]carbamate hydrochloride4-(5-oxo-1,4-diazepan-1-yl)benzoic acid3H-Pyrazol-3-one,1,2-dihydro-5-[2-(methylthio)ethyl]-4-[(4-aminocyclohexyl)methyl]cyclohexan-1- hexane-1,6- 5-isocyanato-1-(isocyanatomethyl)-1,3,3-trimethyl-cyclohexane5(R),11(R)-Diethyl-5,6,11,12-tetrahydrochrysene-2,8-diolL-Lysinamide,N-(phenylacetyl)-L-tyrosyl-D-arginyl-L-a-aspartyl-L-alanyl-L-isoleucyl-4-chloro-L-phenylalanyl-L-threonyl-L-asparaginyl-L-arginyl-L-tyrosyl-L-arginyl-L-lysyl-L-valyl-L-leucyl-(2S)-2-aminobutanoyl-L-glutaminyl-L-leucyl-L-seryl-L-alanyl-L-arginL-Lysinamide,N-(2-phenylacetyl)-L-tyrosyl-D-arginyl-L-a-aspartyl-L-alanyl-L-isoleucyl-4-chloro-L-phenylalanyl-L-threonyl-L-asparaginyl-N6-(aminoiminomethyl)-L-lysyl-O-methyl-L-tyrosyl-L-arginyl-L-lysyl-L-valyl-L-leucyl-(2S)-2-aminobutanoyl-L-glutaminyl-L-Propanamide,2-amino-N,N-diethyl-Propanamide,2-amino-N,N-diethyl-, (2R)-2-Oxiranecarboxylicacid, 3-cyclopropyl-, ethyl ester, (2S,3R)-1,2,4-Oxadiazol-3-ol,5-amino-1,2,4-Oxadiazol-3-ol,4,5-dihydro-5-imino-ethyl 2-[3-acetamido-4-(6-bromo-2-methyl-1,3-dioxo-isoindolin-5-yl)azo-N-ethyl-anilino]propanoateQuino[2,3-b]acridine-7,14-dione,5,12-dihydro-5,12-diphenyl-Furo[2,3-b]quinolin-4(9H)-one,6-hydroxy-9-methyl-Phosphine,1,1'-[2,7-bis(1,1-dimethylethyl)-9,9-dimethyl-9H-xanthene-4,5-diyl]bis[1,1-diphenyl-2H-Tetrazole-2-carboxamide,N,N,5-trimethyl-1H-Tetrazole-1-carboxamide,N,N,5-trimethyl-3H-1,2,4-Triazole-3-thione,1,2-dihydro-5-(1-hydroxyethyl)-3-Penten-2-one,4-(2-propen-1-ylamino)-, (3Z)-4-[(4-ethyl-2,6-difluorophenyl)ethynyl]-4'-propylbiphenylCyclohexanecarbonitrile,1-amino-4-hydroxy-1H-Imidazol-2-amine,4,5-dihydro-N-[4-[[4-(1-methylethoxy)phenyl]methyl]phenyl]-(2E)-1,2,6,7-tetrahydro-8H-indeno[5,4-b]furan-8-ylideneethanenitrile1-Piperidinecarboxylic acid, 4-[(4-aminophenyl)methyl]-,1,1-dimethylethyl esterCarbamic acid,(5-fluoro-2-methylphenyl)-, 1,1-dimethylethyl ester (9CI)3(2H)-Quinazolineaceticacid, 1,4-dihydro-a,a-dimethyl-2,4-dioxo-1H,5H-Dipyrrolo[1,2-a:2',1'-d][1,3,5]triazine(9CI)1H-Benzimidazole,6-chloro-2,5-dimethyl-1H-Benzimidazole,2-cyclopentyl-6-methyl-1H-Benzimidazole,2-cyclopropyl-6-methyl-(2S)-N-[(3S)-1-benzyl-4-[[2-(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-pentyl]-2-(4-hydroxy-2-oxo-hexahydropyrimidin-1-yl)-3-methyl-butanamide2-Butanol,3-amino-1,1-dimethoxy-3-methyl-4-Thiazolecarboxaldehyde,5-bromo-2-methyl-Thiazolo[5,4-c]isoxazole,3,5-dimethyl-6-fluoro-3-methyl-1,2-benzisoxazol-5-amine2-(4-甲磺酰基苯基)-1-(6-甲基吡啶-3-基)-乙酮2-(4-MESYLPHENYL)-1-(6-METHYLPYRIDIN-3-YL)- ETHAN-1-ONE3-Pyridinecarboxamide, N-methoxy-N,6-dimethyl-Acusol 8307-Oxabicyclo[4.1.0]heptan-2-ol,6-methyl-5-bromo-1-phenyl-1H-benzimidazolePyrimidine,2-chloro-5-heptyl-Benzonitrile,4-(1,3-butadiyn-1-yl)-2-Benzothiazolamine,6-fluoro-N-methyl-2-Benzothiazolemethanamine,a,4-dimethyl-, (aR)-2-Benzothiazolemethanamine,4-methyl-a-(1-methylethyl)-, (aR)-2-Benzothiazolemethanamine,6-fluoro-a-methyl-, (aS)-(3Z)-5-{(1S,2R,3R,5S)-3,5-dihydroxy-2-[(1E,3S)-3-hydroxyoct-1-en-1-yl]cyclopentyl}pent-3-enoic acid1H-Pyrrole,1-ethyl-2-nitro-1H-Indole,3-fluoro-5-methyl-1H-Indole,3-fluoro-1-methyl-Phenol,4-[(2S,3S)-2,3-dihydro-3-methyl-5-(1E)-1-propen-1-yl-2-benzofuranyl]-Phenol,4-[(1S)-1-aminoethyl]-7-氮杂吲哚-2-甲酸乙酯ethyl 1H-pyrrolo[2,3-b]pyridine-2-carboxylateBenzenepropanoic acid, b-(acetyloxy)-a,a-dimethyl-3-Pyridinemethanamine, a,6-dimethyl-, (aS)-1H-Indazol-4-amine,7-methyl-1H-Indazol-5-amine,3-fluoro-1H-Indazol-5-amine, 6-chloro-1H-Indazol-6-amine,4-chloro-1H-Indazol-7-amine,5-methyl-1H-Indazol-7-amine,6-methyl-Hydrazine,(4-chloro-3-methylphenyl)-, hydrochloride (1:1)b-D-Glucopyranoside, methyl2-amino-2-deoxy-1-thio-2-Piperidinecarboxamide,1-acetyl-N-methyl-1(2H)-Naphthalenone,3,4-dihydro-8-methyl-, oxime3H-2,1-Benzoxathiole,3a,4,7,7a-tetrahydro-7-methyl-, 1,1-dioxide, (3aR,7aR)-rel-1-Azabicyclo[2.2.2]octane-2-methanol,5-ethynyl-, (1S,2S,4S,5R)-4(1H)-Pyridinone,2-ethyl-3-hydroxy-6-[(2-hydroxyethyl)thio]-tert-butyl N-[(3R)-2-oxo-3-piperidyl]carbamateBenzamide,N-(3-amino-4-methylphenyl)-3-Pyrrolidinemethanol,4-(methylamino)-5-(1-methylethyl)-, (3R,4R,5S)-Fmoc-.alpha.-allyl-DL-Gly-OH1-Naphthalenecarboxaldehyde,7-ethoxy-1,2,3,4-tetrahydro-Imidazo[1,2-a]pyridine-3-carboxylicacid, 2-amino-, ethyl esterBenzene-1,2,3,4-d4,5-chloro-6-[2,2,2-trichloro-1-(4-chlorophenyl-2,3,5,6-d4)ethyl]- (9CI)3-Benzofuranmethanol,6-hydroxy-[8-(2-amino-6-oxo-1H-purin-9-yl)-9-(2-methylaminobenzoyl)oxy-3-oxo-2,4,7-trioxa-3$l^{5}-phosphabicyclo[4.3.0]nonan-3-yl]oxysodiumsodium 4-{[(4-azido-2,3,5,6-tetrafluorophenyl)carbonyl]oxy}-2,3,5,6-tetrafluorobenzenesulfonate氰基亚氨基二苄CyanoiminodibenzylCyclohexanemethanol,2-(1-methylethyl)-Butanoic acid,(2R)-2-pyrrolidinyl ester (9CI)Ethanone,1-[(2R)-2-(acetyloxy)-1-pyrrolidinyl]-Butanoic acid,(2S)-2-pyrrolidinyl ester (9CI)Ethanone,1-[(2S)-2-(acetyloxy)-1-pyrrolidinyl]-L-Prolinamide,N-(1-oxooctadecyl)-L-tyrosylglycyl-L-tyrosyl-L-arginyl-L-leucyl-L-arginyl-L-arginyl-L-lysyl-L-tryptophyl-L-a-glutamyl-L-a-glutamyl-L-lysyl-L-isoleucyl-L-prolyl-L-asparaginyl-(9CI)Acetamide,2-hydroxy-N-methyl-N-(2-oxoethyl)-5-溴-4-氯-4,5,5-三氟-1-戊醇5-bromo-4-chloro-4,5,5-trifluoro-1-pentanol2-methoxy-5-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenyl dihydrogen phosphateAcetamide,N-6-benzothiazolyl-2-(hydroxyimino)-8-(methylsulfanyl)-6,8-dihydro-7H-[1,3]thiazolo[5,4-e]indol-7-one7H-Pyrrolo[2,3-g]benzothiazol-7-one,6,8-dihydro-1H-Indole-2,3-dione,4-(2-methyl-1-buten-1-yl)-1H-Indole-2,3-dione,4-(2-methyl-2-buten-1-yl)-1H-Indole-2,3-dione,4-(cyclobutylidenemethyl)-5-amino-2,3-dihydro-1H-isoindol-1-one2-Pyridinamine,6-methyl-N-2-propen-1-yl-3-Thiophenecarboxylicacid, tetrahydro-2-oxo-2-Thiophenecarboxylicacid, tetrahydro-5-oxo-2H-Thiopyran-2-carboxylicacid, tetrahydro-6-oxo-Pyrazine,2,6-bis(1-methylethyl)-N'-(6-chloro-2-methoxyacridin-9-yl)-N-{3-[(6-chloro-2-methoxyacridin-9-yl)amino]propyl}-N-(3-methoxybenzyl)propane-1,3-diamineCarbamic acid,1H-imidazo[1,2-b]pyrazol-7-yl-, methyl ester (9CI)N-(5-Aminopentyl)maleimide trifluoroacetate salt2,6-Naphthyridine,2-oxideSpiro[bicyclo[2.2.1]heptane-2,5'-oxazolidin]-2'-one,1,7,7-trimethyl-, (1R,2R,4R)-1-Pyrrolidinecarboxylicacid, 2-methyl-, methyl ester3'-formylbiphenyl-3-carboxylic acid4'-formylbiphenyl-3-carboxylic acid3'-formylbiphenyl-4-carboxylic acid2-Thiophenecarboxylicacid, 5-(3-formylphenyl)-2-Thiophenecarboxylicacid, 5-(4-formylphenyl)-Spiro[3,6-dioxabicyclo[3.1.0]hexane-2,3'-pyrrolidine](9CI)1H-Benzothiazolo[4,5,6-ij][2,7]naphthyridine(9CI)4-Pyridinecarboxaldehyde,3-methyl-, oxime2-Pyrrolidinone,3-amino-4-ethyl-, (3S,4R)-Propanal, 2-hydroxy-,2,2-dimethylhydrazoneButanedioic acid,2,3-difluoro-, 1,4-dimethyl ester, (2S,3S)-Cyclohexanone,5-methyl-2-(1-methylethyl)-, hydrazone, (1E,2R,5S)-rel-Ethanone,1-(2-benzoxazolyl)-2,2,2-trifluoro-5-bromo-2-(2-methylpropoxy)benzaldehydeQuinoline,2-methoxy-3-methyl-Quinoline,2,6-diethoxy-9H-Fluorene-2,7-diamine,9,9-dimethyl-N2,N7-di-1-naphthalenyl-N2,N7-diphenyl-Carbamic acid,N-(4-nitrosophenyl)-, methyl ester(1R,5S,6S)-2-[5(S)-[3(S)-(2-Guanidinoacetamido)pyrrolidin-1-ylcarbonyl]-1-methylpyrrolidin-3(S)-ylsulfanyl]-6-[1(R)-hydroxyethyl]-1-methyl-1-carba-2-penem-3-carboxylic acidBenzo[a]benzo[5,6]quino[3,2-i]acridine-9,18-dione,7,16-dihydro-7,16-dimethyl-4H-Pyran-4-one,5-acetyl-2,3-dihydro-2,2-dimethyl-2,3-Pentanedione,4-methyl-, 2-hydrazone, 3-(O-methyloxime)Acetamide,N-(6-fluoro-1H-inden-3-yl)-Acetamide,N-2H-1-benzopyran-4-yl-Acetamide,N-(3,4-dihydro-2-naphthalenyl)-Acetamide,N-(2-methyl-1H-inden-3-yl)-Acetamide,N-(5-fluoro-2,3-dihydro-1H-inden-1-yl)-, (+)-2-Propenoic acid, butylester, homopolymer, reaction products with N1,N1-dimethyl-1,3-propanediamine2-Propenoic acid,2-methyl-, butyl ester, polymer with 2-(dimethylamino)ethyl2-methyl-2-propenoate, 2-[2-(2-ethoxyethoxy)ethoxy]ethyl 2-methyl-2-propenoate,2-ethylhexyl 2-methyl-2-propenoate, methyl 2-methyl-2-propenoate andphenylmethyl 2-methyl-2-propenoa1,2,5-Oxadiazole-3-carboxylicacid, ethyl ester, 2-oxide1H-Pyrrole-2-carboxylicacid, 4-cyano-2,3-dihydro-, methyl ester1H-Pyrrole-2-carboxylicacid, 4-acetyl-2,3-dihydro-, methyl ester1H-Pyrrole-2-carboxylicacid, 4-formyl-2,3-dihydro-, methyl ester2-fluoro-1-methoxy-4-prop-2-en-1-ylbenzene2-Pyrrolidinone,1-ethyl-4-methyl-Methanone,(3-methylene-1-azetidinyl)phenyl-Benzene,1-(3-butyn-1-yl)-4-fluoro-2-Thiabicyclo[3.1.0]hexane-4,6-dicarboxylicacid, 4-amino-, (1R,4S,5S,6S)-2-Thiabicyclo[3.1.0]hexane-4,6-dicarboxylicacid, 4-amino-, (1R,4S,5S,6S)-rel-(+)-(1R,3S)-3-[(tert-butoxycarbonyl)amino]cyclohexanecarboxylic acid1-92-LFA-3 (antigen)(human) fusion protein with immunoglobulin G1 (human hinge-CH2-CH3 g1-chain), dimer (9CI)4-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl chloride2-Pyridinol,3,5-dinitro-1,3-Isobenzofurandione,5-(bromomethyl)-Methanimidamide,N,N-dimethyl-N'-4-pyrimidinyl-3-carboxy-4-[6-(diethylamino)-3-(diethyliminio)-3H-xanthen-9-yl]benzoate2-(chloromethyl)-6-(4-fluorophenyl)pyridine阿哆嗪Adoprazine2-(4-fluorophenyl)-4-methylpyridine1H-Pyrrole-2-carboxaldehyde,5-acetyl-1-methyl-2-Furanacetic acid,5-acetyl-2-Thiophenecarboxaldehyde,4-(methylthio)-(1R,2S)-1,2-diphenyl-2-(propan-2-ylamino)ethanol1-bromo-2,3-dimethoxynaphthaleneethyl (2S)-2-ethoxy-3-(4-hydroxyphenyl)propanoate2-Aziridinecarboxylicacid, 2-(1-methylethylidene)hydrazide, (2S)-Ethanaminium,2-[(2,6-dimethylphenyl)amino]-N,N-diethyl-2-oxo-N-(phenylmethyl)-, hydroxide(1:1)1,3-Dioxolane,2-ethenyl-4-methyl-4-(2-propen-1-yl)-3a(1H)-Pentalenol,3-ethynylhexahydro-, (3R,3aS,6aR)-rel-3a(1H)-Pentalenol,3-ethynylhexahydro-, (3R,3aR,6aS)-rel-2-Propyn-1-ol,3-[2-(1-methylethyl)phenyl]-Carbamic acid,4,6-heptadienyl-, 1,1-dimethylethyl ester (9CI)Thiazolo[5,4-c]isoxazole(9CI)
<FONT color=# 版权所有 &&&京ICP备号&ThedesignandsynthesisofaseriesofnovelinhibitorsofproteinkinaseC(PKC)isdescribed.These2,3-bisarylmaleimideswerederivedfromthestructuralleadprovidedbytheindolocarbazoles,staurosporineandK252a.OptimumactivityrequiredtheimideNH,bothcarbonylgroups,andtheolefinicbondofthemaleimidering.2,3-Bisindolylmaleimideswerethemostactive,andthepotencyofthesewasimprovedbyachlorosubstituentatthe5-positionofoneindolering(compound28,IC500.11microM).Inaseriesof(phenylindolyl)maleimides,nitrocompound74wasmostactive(IC500.67microM).Naphthalene19andbenzothiophene21showedgreaterthan100-foldselectivityforinhibitionofPKCoverthecloselyrelatedcAMP-dependentproteinkinase(PKA).
ThedesignandsynthesisofaseriesofnovelinhibitorsofproteinkinaseC(PKC)isdescribed.These2,3-bisarylmaleimideswerederivedfromthestructuralleadprovidedbytheindolocarbazoles,staurosporineandK252a.OptimumactivityrequiredtheimideNH,bothcarbonylgroups,andtheolefinicbondofthemaleimidering.2,3-Bisindolylmaleimideswerethemostactive,andthepotencyofthesewasimprovedbyachlorosubstituentatthe5-positionofoneindolering(compound28,IC500.11microM).Inaseriesof(phenylindolyl)maleimides,nitrocompound74wasmostactive(IC500.67microM).Naphthalene19andbenzothiophene21showedgreaterthan100-foldselectivityforinhibitionofPKCoverthecloselyrelatedcAMP-dependentproteinkinase(PKA).
被引量:198来源:万方
ABSTRACTAsimplifiedapproachtothesynthesisof2-polyaminelinked-monoindolylmaleimideshasbeenachieved,leadingtoanewseriesoftrypanothionereductaseinhibitors.TheconditionsofaccesstoN,2-bis(polyamine)-3-monoindolylmaleimidesandN,N'-bis(monoindolylmaleimide)polyaminesaredescribed.MeasuredinhibitoryactivitiestowardstrypanothionereductasefromTryanosomacruzishowtheimportanceofbotharomaticmoietiesandpolyaminechainsfortrypanothionereductaserecognition.
ABSTRACTAsimplifiedapproachtothesynthesisof2-polyaminelinked-monoindolylmaleimideshasbeenachieved,leadingtoanewseriesoftrypanothionereductaseinhibitors.TheconditionsofaccesstoN,2-bis(polyamine)-3-monoindolylmaleimidesandN,N'-bis(monoindolylmaleimide)polyaminesaredescribed.MeasuredinhibitoryactivitiestowardstrypanothionereductasefromTryanosomacruzishowtheimportanceofbotharomaticmoietiesandpolyaminechainsfortrypanothionereductaserecognition.
被引量:21来源:Wiley
ABSTRACTDiabetesisachronicmetabolicdisorderthatcontinuestopresentasamajorhealthproblemworldwide.Itischaracterizedbyabsoluteorrelativedeficienciesininsulinsecretionand/orinsulinactionandisassociatedwithchronichyperglycemiaanddisturbancesofcarbohydrate,lipid,andproteinmetabolism.Manystudiessuggestacentralroleforoxidativestressinthepathogenesisofthismulti-facetedmetabolicdisorder.Thishaspromptedinvestigationsintheuseofantioxidantsasacomplementarytherapeuticapproach.Inthisreviewwebrieflysummarizeoxidativemechanismsimplicatedindiabeticcomplicationsandthenfocusonthefindingsresultingfromhumanclinicaltrialswhereantioxidantswerestudiedasanadjuvanttostandarddiabetestreatmentduringthelasttenyears.AliteraturesearchusingPubMed(lasttenyears)wasperformedusingthefollowingterms:vitaminE,vitaminC,coenzymeQ10,alphalipoicacid,L-carnitine,ruboxistaurinorLY333531anddiabetes.Thissearchwaslimitedtohumanclinicaltrials.Weconcludedthereisnotanyestablishedbenefitforantioxidantsuseinthemanagementofdiabeticcomplications.Therefore,routinevitaminormineralsupplementationisnotgenerallyrecommended.
ABSTRACTDiabetesisachronicmetabolicdisorderthatcontinuestopresentasamajorhealthproblemworldwide.Itischaracterizedbyabsoluteorrelativedeficienciesininsulinsecretionand/orinsulinactionandisassociatedwithchronichyperglycemiaanddisturbancesofcarbohydrate,lipid,andproteinmetabolism.Manystudiessuggestacentralroleforoxidativestressinthepathogenesisofthismulti-facetedmetabolicdisorder.Thishaspromptedinvestigationsintheuseofantioxidantsasacomplementarytherapeuticapproach.Inthisreviewwebrieflysummarizeoxidativemechanismsimplicatedindiabeticcomplicationsandthenfocusonthefindingsresultingfromhumanclinicaltrialswhereantioxidantswerestudiedasanadjuvanttostandarddiabetestreatmentduringthelasttenyears.AliteraturesearchusingPubMed(lasttenyears)wasperformedusingthefollowingterms:vitaminE,vitaminC,coenzymeQ10,alphalipoicacid,L-carnitine,ruboxistaurinorLY333531anddiabetes.Thissearchwaslimitedtohumanclinicaltrials.Weconcludedthereisnotanyestablishedbenefitforantioxidantsuseinthemanagementofdiabeticcomplications.Therefore,routinevitaminormineralsupplementationisnotgenerallyrecommended.
被引量:89
ABSTRACTOnwithdrawalfromopioidsmanypatientsexperienceaheightenedsensitivitytostimuliandanexaggeratedpainresponse.Thephenomenonhasbeenlittlestudiedininfants.Wepresentevidencethatinpostnatalday7ratsanexaggeratednociceptiveventralrootresponseofspinalcordsinvitroandwithdrawal-associatedthermalhyperalgesiainvivoaredependentonproteinkinaseC(PKC),andwedocumenttherolesofPKCandgammaisozymes.Invitro,theslowventralrootpotential(sVRP)isanociceptive-relatedresponseinspinalcordthatisdepressedbymorphineandrecoverstolevelssignificantlyabovecontrolonadministrationofnaloxone.Abroad-spectrumPKCantagonist,GF109213X,blockedwithdrawalhyperresponsivenessofthesVRPwhereasanantagonistspecifictoCa(++)-dependentisozymes,Go69076,didnot.Consistentwiththisfinding,aspecificpeptideinhibitorofcalcium-independentPKC,butnotaninhibitorofcalcium-dependentPKCgamma,blockedwithdrawalhyperresponsivenessofthesVRP.Similarly,invivoin7-day-oldratpups,inhibitionofPKC,butnotPKCgamma,preventedthermalhyperalgesiaprecipitatedbynaloxoneat30minpost-morphine.Incontrast,thermalhyperalgesiaduringspontaneouswithdrawalwasinhibitedbybothPKCandgammainhibitors.Theconsistencybetweentheinvivoandinvitrofindingswithrespecttonaloxone-precipitatedwithdrawalprovidesfurtherevidencethatthesVRPreflectsnociceptiveneurotransmission.Ina
ABSTRACTOnwithdrawalfromopioidsmanypatientsexperienceaheightenedsensitivitytostimuliandanexaggeratedpainresponse.Thephenomenonhasbeenlittlestudiedininfants.Wepresentevidencethatinpostnatalday7ratsanexaggeratednociceptiveventralrootresponseofspinalcordsinvitroandwithdrawal-associatedthermalhyperalgesiainvivoaredependentonproteinkinaseC(PKC),andwedocumenttherolesofPKCandgammaisozymes.Invitro,theslowventralrootpotential(sVRP)isanociceptive-relatedresponseinspinalcordthatisdepressedbymorphineandrecoverstolevelssignificantlyabovecontrolonadministrationofnaloxone.Abroad-spectrumPKCantagonist,GF109213X,blockedwithdrawalhyperresponsivenessofthesVRPwhereasanantagonistspecifictoCa(++)-dependentisozymes,Go69076,didnot.Consistentwiththisfinding,aspecificpeptideinhibitorofcalcium-independentPKC,butnotaninhibitorofcalcium-dependentPKCgamma,blockedwithdrawalhyperresponsivenessofthesVRP.Similarly,invivoin7-day-oldratpups,inhibitionofPKC,butnotPKCgamma,preventedthermalhyperalgesiaprecipitatedbynaloxoneat30minpost-morphine.Incontrast,thermalhyperalgesiaduringspontaneouswithdrawalwasinhibitedbybothPKCandgammainhibitors.Theconsistencybetweentheinvivoandinvitrofindingswithrespecttonaloxone-precipitatedwithdrawalprovidesfurtherevidencethatthesVRPreflectsnociceptiveneurotransmission.Ina
被引量:58来源:NCBI
InhibitorsoftheG(2)DNAdamagecheckpointcanselectivelysensitizecancercellswithmutatedp53tokillingbyDNA-damagingagents.IsogranulatimideisaG(2)checkpointinhibitorcontainingauniqueindole/maleimide/imidazoleskeletonidentifiedinaphenotypiccell-however,themechanismofactionofisogranulatimideisunknown.Usingnaturalandsyntheticisogranulatimideanalogues,weshowthattheimidenitrogenandabasicnitrogenatposition14or15intheimidazoleringareimportantforcheckpointinhibition.IsogranulatimideshowsstructuralresemblancetotheaglyconofUCN-01,apotentbisindolemaleimideinhibitorofproteinkinaseCbeta(IC(50),0.001micromol/L)andofthecheckpointkinaseChk1(IC(50),0.007micromol/L).InvitrokinaseassaysshowthatisogranulatimideinhibitsChk1(IC(50),0.1micromol/L)butnotproteinkinaseCbeta.Of13additionalproteinkinasestested,isogranulatimidesignificantlyinhibitsonlyglycogensynthasekinase-3beta(IC(50),0.5micromol/L).WedeterminedthecrystalstructureoftheChk1catalyticdomaincomplexedwithisogranulatimide.LikeUCN-01,isogranulatimidebindsintheATP-bindingpocketofChk1andhydrogenbondswiththebackbonecarbonyloxygenofGlu(85)andtheamidenitrogenofCys(87).UnlikeUCN-01,thebasicN15ofisogranulatimideinteractswithGlu(17),causingaconformationchangeinthekinaseglycine-richloopthatmaycontributeimportantlytoinhibition.ThemechanismbywhichisogranulatimideinhibitsChk1anditsfavorablekinaseselectivityprofilemakeitapromisingcandidateformodulatingcheckpointresponsesintumorsfortherapeuticbenefit.
InhibitorsoftheG(2)DNAdamagecheckpointcanselectivelysensitizecancercellswithmutatedp53tokillingbyDNA-damagingagents.IsogranulatimideisaG(2)checkpointinhibitorcontainingauniqueindole/maleimide/imidazoleskeletonidentifiedinaphenotypiccell-however,themechanismofactionofisogranulatimideisunknown.Usingnaturalandsyntheticisogranulatimideanalogues,weshowthattheimidenitrogenandabasicnitrogenatposition14or15intheimidazoleringareimportantforcheckpointinhibition.IsogranulatimideshowsstructuralresemblancetotheaglyconofUCN-01,apotentbisindolemaleimideinhibitorofproteinkinaseCbeta(IC(50),0.001micromol/L)andofthecheckpointkinaseChk1(IC(50),0.007micromol/L).InvitrokinaseassaysshowthatisogranulatimideinhibitsChk1(IC(50),0.1micromol/L)butnotproteinkinaseCbeta.Of13additionalproteinkinasestested,isogranulatimidesignificantlyinhibitsonlyglycogensynthasekinase-3beta(IC(50),0.5micromol/L).WedeterminedthecrystalstructureoftheChk1catalyticdomaincomplexedwithisogranulatimide.LikeUCN-01,isogranulatimidebindsintheATP-bindingpocketofChk1andhydrogenbondswiththebackbonecarbonyloxygenofGlu(85)andtheamidenitrogenofCys(87).UnlikeUCN-01,thebasicN15ofisogranulatimideinteractswithGlu(17),causingaconformationchangeinthekinaseglycine-richloopthatmaycontributeimportantlytoinhibition.ThemechanismbywhichisogranulatimideinhibitsChk1anditsfavorablekinaseselectivityprofilemakeitapromisingcandidateformodulatingcheckpointresponsesintumorsfortherapeuticbenefit.
被引量:55
GilbertRE,KimSA,TuttleKR,BakrisGL,TotoRD,McGillJB,HaneyDJ,KellyDJ,AndersonPW.
GilbertRE,KimSA,TuttleKR,BakrisGL,TotoRD,McGillJB,HaneyDJ,KellyDJ,AndersonPW.
被引量:48
Vascularendothelialgrowthfactor(VEGF)isimplicatedinthedevelopmentofproteinuriaindiabeticnephropathy.HighambientglucosepresentindiabetesstimulatesVEGFexpressioninseveralcelltypes,butthemolecularmechanismsareincompletelyunderstood.Hereprimaryculturedratmesangialcellsservedasamodeltoinvestigatethesignaltransductionpathwaysinvolvedinhigh-glucose-inducedVEGFexpression.Exposuretohighglucose(25mM)significantlyincreasedVEGFmRNAevaluatedbyreal-timePCRby3h,VEGFcellularproteincontentassessedbyimmunoblottingorimmunofluorescencewithin24h,andVEGFsecretionby24h.High-glucose-inducedVEGFexpressionwasblockedbyanantioxidant,Tempol,andantisenseoligonucleotidesdirectedagainstp22(phox),aNADPHoxidasesubunit.InhibitionofproteinkinaseC(PKC)-beta(1)withthespecificpharmacologicalinhibitorLY-333531orinhibitionofPKC-zetawithacellpermeablespecificpseudosubstratepeptidealsopreventedenhancedVEGFexpressioninhighglucose.EnhancedVEGFsecretioninhighglucosewaspreventedbyTempol,PKC-beta(1),orPKC-zetainhibition.Innormalglucose(5.6mM),overexpressionofp22(phox)orconstitutivelyactivePKC-zetaenhancedVEGFexpression.Hypoxiainduciblefactor-1alphaproteinwassignificantlyincreasedinhighglucoseonlyby24h,suggestingapossiblecontributiontohigh-glucose-stimulatedVEGFexpressionatlatertimepoints.ThusreactiveoxygenspeciesgeneratedbyNADPHoxidase,andbothPKC-beta(1)and-zeta,playimportantrolesinhigh-glucose-stimulatedVEGFexpressionandsecretionbymesangialcells.
Vascularendothelialgrowthfactor(VEGF)isimplicatedinthedevelopmentofproteinuriaindiabeticnephropathy.HighambientglucosepresentindiabetesstimulatesVEGFexpressioninseveralcelltypes,butthemolecularmechanismsareincompletelyunderstood.Hereprimaryculturedratmesangialcellsservedasamodeltoinvestigatethesignaltransductionpathwaysinvolvedinhigh-glucose-inducedVEGFexpression.Exposuretohighglucose(25mM)significantlyincreasedVEGFmRNAevaluatedbyreal-timePCRby3h,VEGFcellularproteincontentassessedbyimmunoblottingorimmunofluorescencewithin24h,andVEGFsecretionby24h.High-glucose-inducedVEGFexpressionwasblockedbyanantioxidant,Tempol,andantisenseoligonucleotidesdirectedagainstp22(phox),aNADPHoxidasesubunit.InhibitionofproteinkinaseC(PKC)-beta(1)withthespecificpharmacologicalinhibitorLY-333531orinhibitionofPKC-zetawithacellpermeablespecificpseudosubstratepeptidealsopreventedenhancedVEGFexpressioninhighglucose.EnhancedVEGFsecretioninhighglucosewaspreventedbyTempol,PKC-beta(1),orPKC-zetainhibition.Innormalglucose(5.6mM),overexpressionofp22(phox)orconstitutivelyactivePKC-zetaenhancedVEGFexpression.Hypoxiainduciblefactor-1alphaproteinwassignificantlyincreasedinhighglucoseonlyby24h,suggestingapossiblecontributiontohigh-glucose-stimulatedVEGFexpressionatlatertimepoints.ThusreactiveoxygenspeciesgeneratedbyNADPHoxidase,andbothPKC-beta(1)and-zeta,playimportantrolesinhigh-glucose-stimulatedVEGFexpressionandsecretionbymesangialcells.
被引量:44
AbstractDiabeticretinopathyremainsamajorcauseofworldwidepreventableblindness.Measurestoavoidblindnessincludemedicalmanagement(controlofbloodsugar,bloodpressure,andserumlipids)andocularmanagement(laserphotocoagulationandparsplanavitrectomy).Adjunctivepharmacologictherapies(intravitrealtriamcinoloneacetonideandanti-vascularendothelialgrowthfactoragents)haveshownearlypromiseinthetreatmentofbothdiabeticmacularedemaandproliferativediabeticretinopathy.Othermedicationsunderinvestigationincludethefluocinoloneacetonideimplantabledevice,extended-releasedexamethasoneimplant,oralruboxistaurin,andintravitrealhyaluronidase.
AbstractDiabeticretinopathyremainsamajorcauseofworldwidepreventableblindness.Measurestoavoidblindnessincludemedicalmanagement(controlofbloodsugar,bloodpressure,andserumlipids)andocularmanagement(laserphotocoagulationandparsplanavitrectomy).Adjunctivepharmacologictherapies(intravitrealtriamcinoloneacetonideandanti-vascularendothelialgrowthfactoragents)haveshownearlypromiseinthetreatmentofbothdiabeticmacularedemaandproliferativediabeticretinopathy.Othermedicationsunderinvestigationincludethefluocinoloneacetonideimplantabledevice,extended-releasedexamethasoneimplant,oralruboxistaurin,andintravitrealhyaluronidase.
被引量:37
ABSTRACTBACKGROUND:Curcumin,theactiveingredientofturmeric(Curcumalonga),isknowntohaveanti-inflammatoryandantioxidativeproperties.Thepresentstudywasaimedtodeterminetheeffectofcurcumininregionalmyocardialischemia/reperfusion(I/R)injuryanditsunderlyingmechanismsinvolvingtheroleofprosurvivalkinasesandapoptotickinases.METHODS:Sprague-Dawleyrats(n=109)subjectedtoa30-minuteleftanteriordescendingcoronaryartery(LAD)occlusionfollowedbyreperfusionwereassignedtoreceivesaline(control),curcumin(100mg/kg),wortmannin(inhibitorofphosphatidylinositol-3-OHkinase[PI3K]-Akt),wortmannin+curcumin,U0126(inhibitorofextracellularsignal-regulatedkinase[ERK1/2]),U0126+curcumin,SB216763(inhibitorofglycogensynthasekinase[GSK-3β]),andSB216763+curcumin20minutesbeforeLADocclusion.Infarctsizewasmeasuredafter2hoursofreperfusionbytriphenyltetrazoliumchloridestaining.ThephosphorylationofAkt,ERK1/2,GSK-3β,p38,andc-JunN-terminalkinases(JNK)wasdeterminedbyimmunoblottingaf
ABSTRACTBACKGROUND:Curcumin,theactiveingredientofturmeric(Curcumalonga),isknowntohaveanti-inflammatoryandantioxidativeproperties.Thepresentstudywasaimedtodeterminetheeffectofcurcumininregionalmyocardialischemia/reperfusion(I/R)injuryanditsunderlyingmechanismsinvolvingtheroleofprosurvivalkinasesandapoptotickinases.METHODS:Sprague-Dawleyrats(n=109)subjectedtoa30-minuteleftanteriordescendingcoronaryartery(LAD)occlusionfollowedbyreperfusionwereassignedtoreceivesaline(control),curcumin(100mg/kg),wortmannin(inhibitorofphosphatidylinositol-3-OHkinase[PI3K]-Akt),wortmannin+curcumin,U0126(inhibitorofextracellularsignal-regulatedkinase[ERK1/2]),U0126+curcumin,SB216763(inhibitorofglycogensynthasekinase[GSK-3β]),andSB216763+curcumin20minutesbeforeLADocclusion.Infarctsizewasmeasuredafter2hoursofreperfusionbytriphenyltetrazoliumchloridestaining.ThephosphorylationofAkt,ERK1/2,GSK-3β,p38,andc-JunN-terminalkinases(JNK)wasdeterminedbyimmunoblottingaf
被引量:30来源:NCBI
WehavefoundthatphosphorylationofaG-protein-coupledreceptorbyproteinkinaseC(PKC)disruptsmodulationofionchannelsbythereceptor.InAtT-20cell
WehavefoundthatphosphorylationofaG-protein-coupledreceptorbyproteinkinaseC(PKC)disruptsmodulationofionchannelsbythereceptor.InAtT-20cell
被引量:245
京ICP证030173号}

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