Activation of mitogen activated protein kinase (MAPK) during D-galactosamine intoxication in the rat liver.

Abstract:

:A significant increase in plasma glutamate-oxaloacetate transaminase and glutamate-pyruvate transaminase was observed 6 h after intraperitoneal administration of D-galactosamine (D-Galn). Three hours after administration of D-Galn, the vitamin C concentration in the liver decreased significantly compared to that in a control group and thereafter the hepatic vitamin C concentration remained at a significantly lower level. Phosphorylated JNK (c-Jun NH2-terminal kinase) and phosphorylated ERK (extracellular signal-regulated kinase) started increasing 3 h after D-Galn treatment and remained at a high level for 6-12 h after the treatment, while phosphorylated p38 MAPK increased significantly 6 h after D-Galn administration. These results indicated that oxidative stress and the activation of JNK and ERK took place almost simultaneously, followed by the activation of p38 MAPK.

journal_name

Bioorg Med Chem Lett

authors

Nishioka H,Kishioka T,Iida C,Fujii K,Ichi I,Kojo S

doi

10.1016/j.bmcl.2006.02.057

subject

Has Abstract

pub_date

2006-06-01 00:00:00

pages

3019-22

issue

11

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(06)00243-5

journal_volume

16

pub_type

杂志文章
  • Photo-controlled release of fipronil from a coumarin triggered precursor.

    abstract::Developing efficient controlled release system of insecticide can facilitate the better use of insecticide. We described here a first example of photo-controlled release of an insecticide by linking fipronil with photoresponsive coumarin covalently. The generated coumarin-fipronil (CF) precursor could undergo cleavage...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2017.03.091

    authors: Gao Z,Yuan P,Wang D,Xu Z,Li Z,Shao X

    更新日期:2017-06-01 00:00:00

  • Further constituents of Galianthe thalictroides (Rubiaceae) and inhibition of DNA topoisomerases I and IIα by its cytotoxic β-carboline alkaloids.

    abstract::A new cytotoxic β-carboline alkaloid, 1-methyl-3-(2-hydroxypropan-2-yl)-2-(5-methoxy-9H-β-carbolin-1-yl)-cyclopentanol (1), was isolated from roots of Galianthe thalictroides, together with the alkaloid 1-(hydroxymethyl)-3-(2-hydroxypropan-2-yl)-2-(5-methoxy-9H-β-carbolin-1-yl)-cyclopentanol (2), the anthraquinones 1-...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2014.01.039

    authors: de Oliveira Figueiredo P,Perdomo RT,Garcez FR,de Fatima Cepa Matos M,de Carvalho JE,Garcez WS

    更新日期:2014-03-01 00:00:00

  • Cytotoxicity and DNA binding property of the dimers of triphenylethylene-coumarin hybrid with one amino side chain.

    abstract::Novel dimers of triphenylethylene-coumarin hybrid containing one amino side chain were designed and synthesized by the condensation of four dicarboxylic acids with the amino monomeric hybrids catalyzed by HATU and DIPEA at room temperature. The adding order of the reactants had a significant effect on the condensation...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2014.04.106

    authors: Tan G,Yao Y,Gu Y,Li S,Lv M,Wang K,Chen H,Li X

    更新日期:2014-07-01 00:00:00

  • Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.

    abstract::The synthesis and evaluation of tetrasubstituted aminopyridines, bearing novel azaindazole hinge binders, as potent AKT inhibitors are described. Compound 14c was identified as a potent AKT inhibitor that demonstrated reduced CYP450 inhibition and an improved developability profile compared to those of previously desc...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2009.11.061

    authors: Lin H,Yamashita DS,Xie R,Zeng J,Wang W,Leber J,Safonov IG,Verma S,Li M,Lafrance L,Venslavsky J,Takata D,Luengo JI,Kahana JA,Zhang S,Robell KA,Levy D,Kumar R,Choudhry AE,Schaber M,Lai Z,Brown BS,Donovan BT,Mi

    更新日期:2010-01-15 00:00:00

  • Discovery of a new series of monoamine reuptake inhibitors, the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ols.

    abstract::A novel series of monoamine reuptake inhibitors, the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ols, have been discovered by combining virtual and focused screening efforts with design techniques. Synthesis of the two diastereomeric isomers of the molecule followed by chiral resolution of each enantiomer revealed the ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2009.07.053

    authors: Kim CY,Mahaney PE,McConnell O,Zhang Y,Manas E,Ho DM,Deecher DC,Trybulski EJ

    更新日期:2009-09-01 00:00:00

  • Synthesis of 3-[4-(dimethylamino)phenyl]alkyl-2-oxindole derivatives and their effects on neuronal cell death.

    abstract::Novel 3-[4-(dimethylamino)phenyl]alkyl-2-oxindole analogs were synthesized by either of the following two pathways: (1) a sequence of Knoevenagel condensation of oxindole with (4-dimethylamino)cinnamaldehyde-hydrogenation, or (2) alkylation of oxindole dianion with [(4-dimethylamino)phenyl]alkyl halides. Subsequent al...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2017.08.005

    authors: Furuta K,Kawai Y,Mizuno Y,Hattori Y,Koyama H,Hirata Y

    更新日期:2017-09-15 00:00:00

  • Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.

    abstract::Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites. In order to reduce attrition due to metabolism-induced toxicity and to improve the safety of drug candidates, we developed a simple cell viability assay by combining a bioactivation system (huma...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2016.06.088

    authors: Rana P,Will Y,Nadanaciva S,Jones LH

    更新日期:2016-08-15 00:00:00

  • Identification of quinones as novel PIM1 kinase inhibitors.

    abstract::PIM1 is a proto-oncogene encoding the serine/threonine PIM1 kinase. PIM1 kinase plays important roles in regulating aspects of cell cycle progression, apoptosis resistance, and has been implicated in the development of such malignancies as prostate cancer and acute myeloid leukemia among others. Knockout of PIM1 kinas...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2016.04.079

    authors: Schroeder RL,Goyal N,Bratton M,Townley I,Pham NA,Tram P,Stone T,Geathers J,Nguyen K,Sridhar J

    更新日期:2016-07-01 00:00:00

  • Novel bis(indolyl)hydrazide-hydrazones as potent cytotoxic agents.

    abstract::A series of bis(indolyl) hydrazide-hydrazones 5a-n were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of indole-3-carboxaldehyde 2 with indole-3-carbohydrazide 4 in presence of catalytic amount of acetic acid afforded 5a-n in good yields. Among the synthesized ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2011.11.031

    authors: Kumar D,Maruthi Kumar N,Ghosh S,Shah K

    更新日期:2012-01-01 00:00:00

  • Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors.

    abstract::The structure activity relationship of the prime region of conformationally restricted hydroxyethylamine (HEA) BACE inhibitors is described. Variation of the P1' region provided selectivity over Cat-D with a series of 2,2-dioxo-isothiochromanes and optimization of the P2' substituent of chromane-HEA(s) with polar subs...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2013.06.006

    authors: Ng RA,Sun M,Bowers S,Hom RK,Probst GD,John V,Fang LY,Maillard M,Gailunas A,Brogley L,Neitz RJ,Tung JS,Pleiss MA,Konradi AW,Sham HL,Dappen MS,Adler M,Yao N,Zmolek W,Nakamura D,Quinn KP,Sauer JM,Bova MP,Ruslim

    更新日期:2013-08-15 00:00:00

  • Hydroxyoxazolidines as alpha-aminoacetaldehye equivalents: novel inhibitors of calpain.

    abstract::The synthesis of [1-[(5-hydroxy-4-(phenylmethyl)-3-oxazolidinyl)carbonyl]-2-ethylpropy lcarbamic acid phenylmethyl ester (2; MDL 104,903), a potent inhibitor of calpain, is described. Synthesis of related compounds, which offer insights into the mechanism of action for 2, are also described, as is an O-acetyl prodrug ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/s0960-894x(99)00391-1

    authors: Peet NP,Kim HO,Marquart AL,Angelastro MR,Nieduzak TR,White JN,Friedrich D,Flynn GA,Webster ME,Vaz RJ,Linnik MD,Koehl JR,Mehdi S,Bey P,Emary B,Hwang KK

    更新日期:1999-08-16 00:00:00

  • Derivatization of the C12-C13 functional groups of epothilones A, B and C.

    abstract::Epothilone A reacted with hydrohalic acids to C12-C13 halohydrin regioisomers (ratios: 2:1-4:1), whereas epothilone B gave under the same conditions the isomerically pure C12 halo C13 hydroxy derivative. With non-nucleophilic Brønstedt acids and with Lewis acids a highly solvent dependent product distribution and some...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/S0960-894X(98)00546-0

    authors: Sefkow M,Kiffe M,Höfle G

    更新日期:1998-11-03 00:00:00

  • Folic acid conjugates of a bleomycin mimic for selective targeting of folate receptor positive cancer cells.

    abstract::A major challenge in the application of cytotoxic anti-cancer drugs is their general lack of selectivity, which often leads to systematic toxicity due to their inability to discriminate between malignant and healthy cells. A particularly promising target for selective targeting are the folate receptors (FR) that are o...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2019.05.047

    authors: Geersing A,de Vries RH,Jansen G,Rots MG,Roelfes G

    更新日期:2019-08-01 00:00:00

  • A new backbone of artificial enzymes obtained by cross-linkage of poly(ethylenimine).

    abstract::Cross-linkage of the branches of poly(ethylenimine) (PEI) suppresses flexibility of the polymer as revealed by decreased affinity of the amino groups on PEI backbone towards proton or Ni(II) ion. The cross-linkage improves ability of the PEI derivative equipped with beta-cyclodextrin to deacylate an ester containing t...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/s0960-894x(98)00212-1

    authors: Suh J,Noh YS

    更新日期:1998-06-02 00:00:00

  • Structure-activity relationships in 2-aminodiphenylsulfides against trypanothione reductase from Trypanosoma cruzi.

    abstract::In order to establish structural elements responsible for inhibition of trypanothione reductase (TR) from Trypanosoma cruzi by 2-aminodiphenylsulfides, a series of dissymmetrical derivatives, corresponding to the replacement of one aromatic moiety by different amines, was synthesized. TR inhibition studies revealed th...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/s0960-894x(98)00180-2

    authors: Girault S,Davioud-Charvet E,Salmon L,Berecibar A,Debreu MA,Sergheraert C

    更新日期:1998-05-19 00:00:00

  • Substituent effect on the preferred DNA binding mode and affinity of a homologous series of naphthalene diimides.

    abstract::A combination of isothermal titration calorimetry (ITC), topoisomerase I DNA unwinding assays, and ethidium bromide displacement studies were employed to investigate the binding of a homologous series of naphthalene diimides (NDI) to DNA. Our results suggest that the nature of the substituent plays a significant role ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2011.05.069

    authors: McKnight RE,Reisenauer E,Pintado MV,Polasani SR,Dixon DW

    更新日期:2011-07-15 00:00:00

  • Design and synthesis of new hydroxyethylamines as inhibitors of D-alanyl-D-lactate ligase (VanA) and D-alanyl-D-alanine ligase (DdlB).

    abstract::The Van enzymes are ATP-dependant ligases responsible for resistance to vancomycin in Staphylococcus aureus and Enteroccoccus species. The de novo molecular design programme SPROUT was used in conjunction with the X-ray crystal structure of Enterococcus faeciumd-alanyl-d-lactate ligase (VanA) to design new putative in...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2009.01.034

    authors: Sova M,Cadez G,Turk S,Majce V,Polanc S,Batson S,Lloyd AJ,Roper DI,Fishwick CW,Gobec S

    更新日期:2009-03-01 00:00:00

  • Discovery of 1-(1H-indazol-4-yl)-3-((1-phenyl-1H-pyrazol-5-yl)methyl) ureas as potent and thermoneutral TRPV1 antagonists.

    abstract::A series of 1-indazol-3-(1-phenylpyrazol-5-yl)methyl ureas were investigated as hTRPV1 antagonists. The structure-activity relationship study was conducted systematically for both the indazole A-region and the 3-trifluoromethyl/t-butyl pyrazole C-region to optimize the antagonism toward the activation by capsaicin. Am...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2020.127548

    authors: Kang JM,Kwon SO,Ann J,Blumberg PM,Ha H,Yoo YD,Frank-Foltyn R,Lesch B,Bahrenberg G,Stockhausen H,Christoph T,Lee J

    更新日期:2020-12-01 00:00:00

  • Synthesis of novel chromeno-annulated cis-fused pyrano[3,4-c]benzopyran and naphtho pyran derivatives via domino aldol-type/hetero Diels-Alder reaction and their cytotoxicity evaluation.

    abstract::New chromeno-annulated cis-fused pyrano[3,4-c]benzopyran and naphtho pyran derivatives have been synthesized by domino aldol-type reaction/hetero Diels-Alder reaction generated from o-quinone methide in situ from 7-O-prenyl derivatives of 8-formyl-2,3-disubstituted chromenones with resorcinols/naphthols in the presenc...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2014.08.005

    authors: Madda J,Venkatesham A,Naveen Kumar B,Nagaiah K,Sujitha P,Ganesh Kumar C,Rao TP,Jagadeesh Babu N

    更新日期:2014-09-15 00:00:00

  • Protective effect of nitronyl nitroxide-amino acid conjugates on liver ischemia-reperfusion induced injury in rats.

    abstract::Stable nitroxides are potential antioxidant drugs. In this study, we have linked nitroxide to natural amino acids with the aim to improve therapeutic activity. The radical scavenging activities of two nitronyl nitroxide-amino acid conjugates (NNR and NNK) were evaluated in PC 12 cell survival assays. The NO scavenging...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2008.02.030

    authors: Bi W,Cai J,Xue P,Zhang Y,Liu S,Gao X,Li M,Wang Z,Baudy-Floc'h M,Green SA,Bi L

    更新日期:2008-03-15 00:00:00

  • Isoindol-1,3-dione and isoindol-1-one derivatives with high binding affinity to beta-amyloid fibrils.

    abstract::Based on the structural features of Indoprofen and PIB, a series of isoindol-1,3-diones 1a-k and isoindol-1-ones 2a-l were designed and synthesized. These 23 compounds were evaluated by competitive binding assay against aggregated Abeta42 fibrils using [(125)I]TZDM. All the isoindolone derivatives showed very good bin...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2008.01.066

    authors: Lee HJ,Lim SJ,Oh SJ,Moon DH,Kim DJ,Tae J,Yoo KH

    更新日期:2008-03-01 00:00:00

  • The tert-butyl dimethyl silyl group as an enhancer of drug cytotoxicity against human tumor cells.

    abstract::In this study, we synthesized a series of enantiomerically pure (2R,3S)-disubstituted tetrahydropyranes with diverse functional groups using known methodologies. In addition to the tert-butyl dimethyl silyl group, other common protecting groups for hydroxyl groups such as allyl, acetate, and benzoate were used to obta...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2005.05.126

    authors: Donadel OJ,Martín T,Martín VS,Villar J,Padrón JM

    更新日期:2005-08-01 00:00:00

  • Naphthoquinone analogs as inactivators of cdc25 phosphatase.

    abstract::cdc25A and cdc25B were significantly overexpressed in certain types of cancers, and they represent potential therapeutic targets for anticancer drug. In this study, naphthoquinone analogs as cdc25A phosphatase inactivators were investigated. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/s0960-894x(98)00411-9

    authors: Ham SW,Park J,Lee SJ,Kim W,Kang K,Choi KH

    更新日期:1998-09-22 00:00:00

  • Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.

    abstract::The synthesis and structure-activity relationships (SAR) of novel, potent imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors are described. The X-ray crystal structure of imidazo[1,2-a]pyrazine Aurora inhibitor 1j is disclosed. Compound 10i was identified as lead compound with a promising overall profile. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2010.07.008

    authors: Belanger DB,Curran PJ,Hruza A,Voigt J,Meng Z,Mandal AK,Siddiqui MA,Basso AD,Gray K

    更新日期:2010-09-01 00:00:00

  • Microwave-assisted synthesis of novel 5-substituted benzylidene amino-2-butyl benzofuran-3-yl-4-methoxyphenyl methanones as antileishmanial and antioxidant agents.

    abstract::A series of 5-substitutedbenzylideneamino-2-butylbenzofuran-3-yl-4-methoxyphenyl methanones is synthesized and evaluated for antileishmanial and antioxidant activities. Compounds 4f (IC50 = 52.0 ± 0.09 µg/ml), 4h (IC50 = 56.0 ± 0.71 µg/ml) and 4l (IC50 = 59.3 ± 0.55 µg/ml) were shown significant antileishmanial when c...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2017.12.013

    authors: Patil SR,Bollikonda S,Patil RH,Sangshetti JN,Bobade AS,Asrondkar A,Reddy PP,Shinde DB

    更新日期:2018-02-01 00:00:00

  • Photochemical control of FlAsH labeling of proteins.

    abstract::Spatiotemporal control of protein fluorescence is a powerful tool in tracking protein movements within cells. Here we report an approach to using genetically encoded photo-caged amino acids to control labeling protein tetracysteine tags with biarsenical fluorescein dyes (FlAsH). ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2009.05.072

    authors: Wilkins BJ,Yang X,Cropp TA

    更新日期:2009-08-01 00:00:00

  • Design, synthesis, and antibacterial activity of 2,5-dihydropyrrole formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.

    abstract::The synthesis and antibacterial activity of 2,5-dihydropyrrole formyl hydroxyamino derivatives are reported. The antibacterial activities of these derivatives were evaluated, and some of these derivatives showed better in vitro antibacterial activity than existing drugs, including penicillin, ciprofloxacin, vancomycin...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2010.04.123

    authors: Shi W,Duan Y,Qian Y,Li M,Yang L,Hu W

    更新日期:2010-06-15 00:00:00

  • Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors.

    abstract::Aromatase is a target of pharmacological interest for the treatment of estrogen-dependent cancers. Azole derivatives such as letrozole or anastrozole have been developed for aromatase inhibition and are used for the treatment of breast tumors. In this paper, four 4-triazolylflavans were synthesized and were found to e...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2004.07.090

    authors: Yahiaoui S,Pouget C,Fagnere C,Champavier Y,Habrioux G,Chulia AJ

    更新日期:2004-10-18 00:00:00

  • Identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors.

    abstract::Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway is one of the most intensively studied approaches to cancer therapy. Rational design led to the identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibito...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2013.12.112

    authors: Lin S,Han F,Liu P,Tao J,Zhong X,Liu X,Yi C,Xu H

    更新日期:2014-02-01 00:00:00

  • Structure-based design and subsequent optimization of 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) inhibitors of p38 MAP kinase.

    abstract::A computer-aided drug design strategy leads to the identification of a new class of p38 inhibitors based on the 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) scaffold. The tolyl triazole amides provided a potent platform amenable to optimization. Further exploration leads to compounds with greater than 100-fold improveme...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章

    doi:10.1016/j.bmcl.2008.04.043

    authors: Cogan DA,Aungst R,Breinlinger EC,Fadra T,Goldberg DR,Hao MH,Kroe R,Moss N,Pargellis C,Qian KC,Swinamer AD

    更新日期:2008-06-01 00:00:00