Synthesis of indomethacin analogues for evaluation as modulators of MRP activity.

abstract：:Versatile method for living cell labeling has been established. Cell surfaces are initially biotinylated by azaelectrocyclization, and then treated with the fluorescence-labeled avidin or the anti-biotin antibody. ...

journal_title：Bioorganic & medicinal chemistry

authors： Tanaka K,Yokoi S,Morimoto K,Iwata T,Nakamoto Y,Nakayama K,Koyama K,Fujiwara T,Fukase K

更新日期：2012-03-15 00:00:00

abstract：:Phosphoinositide 3-kinases (PI3-Ks) are an ubiquitous class of signaling enzymes that regulate diverse cellular processes including growth, differentiation, and motility. Physiological roles of PI3-Ks have traditionally been assigned using two pharmacological inhibitors, LY294002 and wortmannin. Although these compoun...

journal_title：Bioorganic & medicinal chemistry

authors： Knight ZA,Chiang GG,Alaimo PJ,Kenski DM,Ho CB,Coan K,Abraham RT,Shokat KM

更新日期：2004-09-01 00:00:00

abstract：:The molecular structure of 2alpha-hydroxyneoanisatin, a positional isomer of the potent neurotoxin anisatin, was determined by X-ray crystallographic analysis. This compound and four further seco-prezizaane type sesquiterpene lactones previously isolated from Illicium floridanum, which represent different structural t...

journal_title：Bioorganic & medicinal chemistry

authors： Schmidt TJ,Okuyama E,Fronczek FR

更新日期：1999-12-01 00:00:00

abstract：:Compounds that bind at the colchicine site of tubulin have drawn considerable attention with studies indicating that these agents suppress microtubule dynamics and inhibit tubulin polymerization. Data for 18 polysubstituted pyrrole compounds are reported, including antiproliferative activity against human MDA-MB-435 c...

journal_title：Bioorganic & medicinal chemistry

authors： Tripathi A,Fornabaio M,Kellogg GE,Gupton JT,Gewirtz DA,Yeudall WA,Vega NE,Mooberry SL

更新日期：2008-03-01 00:00:00

abstract：:To discover new inhibitors on tissue factor procoagulant activity, 21 tetrahydroprotoberberines were screened on the model of human THP-1 cells stimulated by lipopolysaccharide. Among these tetrahydroprotoberberines, several unique compounds were synthesized through microbial transformation: compound 6 (l-corydalmine)...

journal_title：Bioorganic & medicinal chemistry

authors： Ge HX,Zhang J,Chen L,Kou JP,Yu BY

更新日期：2013-01-01 00:00:00

abstract：:The substitution of the sterically hindered carbon of the potent thyroid hormone agonist, GC-1, was effected by a reaction based on the solvolysis of the benzylic hydroxyl group. The reaction was found to proceed in high yield with a variety of nucleophiles including alcohols, thiols, allyl silanes and electron-rich a...

journal_title：Bioorganic & medicinal chemistry

authors： Yoshihara HA,Chiellini G,Mitchison TJ,Scanlan TS

更新日期：1998-08-01 00:00:00

abstract：:A new class of compounds able to block the replication of subgenomic HCV RNA in liver cells is described. 3-Amino-2(5H)furanones 4 may be regarded as diketoacid analogues and were obtained by basic rearrangement of the isoxazolidine nucleus. ...

journal_title：Bioorganic & medicinal chemistry

authors： Iannazzo D,Piperno A,Romeo G,Romeo R,Chiacchio U,Rescifina A,Balestrieri E,Macchi B,Mastino A,Cortese R

更新日期：2008-11-01 00:00:00

abstract：:The purpose of this study was to synthesize two new positron emission tomography (PET) probes, N-(4-(2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl)phenyl)-9,10-dihydro-5-[¹⁸F]fluoroethoxy-9-oxo-4-acridine carboxamide ([¹⁸F]3) and quinoline-3-carboxylic acid [2-(4-{2-[7-(2-[¹⁸F]fluoroethoxy)-6-methoxy-3,4-d...

journal_title：Bioorganic & medicinal chemistry

authors： Kawamura K,Yamasaki T,Konno F,Yui J,Hatori A,Yanamoto K,Wakizaka H,Ogawa M,Yoshida Y,Nengaki N,Fukumura T,Zhang MR

更新日期：2011-01-15 00:00:00

abstract：:A series of 40 7-(O-substituted)-2-morpholino-8-aryl-4H-benzo[e][1,3]oxazin-4-one derivatives was synthesized. They were prepared via synthesis of a key precursor, 8-bromo-7-hydroxy-2-morpholino-4H-benzo[e][1,3]oxazin-4-one 13 which was amenable to ether synthesis at the 7-position and Suzuki coupling at the 8-positio...

journal_title：Bioorganic & medicinal chemistry

authors： Saifuzzaman M,Morrison R,Zheng Z,Orive S,Hamilton J,Thompson PE,Al-Rawi JMA

更新日期：2017-10-15 00:00:00

abstract：:Activation of the nuclear farnesoid X receptor (FXR) which acts as cellular bile acid sensor has been validated as therapeutic strategy to counter liver disorders such as non-alcoholic steatohepatitis by the clinical efficacy of obeticholic acid. FXR antagonism, in contrast, is less well studied and potent small molec...

journal_title：Bioorganic & medicinal chemistry

authors： Schmidt J,Schierle S,Gellrich L,Kaiser A,Merk D

更新日期：2018-08-07 00:00:00

abstract：:Seven new triterpenoid saponins (1-7), have been isolated and elucidated from the roots of Gypsophila oldhamiana together with five known triterpenoid saponins (8-12). These saponins which could be classified into three series: 3-O-monoglucosides (1, 8, 9), 28-O-monoglucosides (2-4, 12) and 3, 28-O-bidesmosides (5-7, ...

journal_title：Bioorganic & medicinal chemistry

authors： Luo JG,Ma L,Kong LY

更新日期：2008-03-15 00:00:00

abstract：:Synthesis and in vitro cytotoxicity assays of new anthranilamide MDR modulators have been performed to assess their inhibition potency on the P-glycoprotein (P-gp) transporter. Previous studies showed that the replacement of the aromatic spacer group between nitrogen atoms (N(1) and N(2)) in the P-gp inhibitor XR9576 ...

journal_title：Bioorganic & medicinal chemistry

authors： Labrie P,Maddaford SP,Lacroix J,Catalano C,Lee DK,Rakhit S,Gaudreault RC

更新日期：2007-06-01 00:00:00

abstract：:Antibiotic resistance among clinically significant bacterial pathogens, such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant S. aureus (VRSA) is becoming a prevalent threat to public health, and new antibacterial agents with novel mechanisms of action hence are in an urgent need. As a pa...

journal_title：Bioorganic & medicinal chemistry

authors： Song D,Bi F,Zhang N,Qin Y,Liu X,Teng Y,Ma S

更新日期：2020-11-01 00:00:00

abstract：:The two-metal binding model we previously reported as an inhibition mechanism of HIV integrase (HIV IN) produced a new direction in modification of 2-hydroxy-3-heteroaryl acrylic acid inhibitors (HHAAs). Here we present a novel series of HIV IN inhibitors having a 3-hydroxy-1,5-dihydro-pyrrol-2-one moiety (HDPO) as an...

journal_title：Bioorganic & medicinal chemistry

authors： Kawasuji T,Fuji M,Yoshinaga T,Sato A,Fujiwara T,Kiyama R

更新日期：2007-08-15 00:00:00

abstract：:A series of 3- and 4-(sulfo- and sulfonamidoalkyl)pyridine and piperidine-2-carboxylic acid derivatives as analogs of NMDA receptor antagonists was prepared. Affinity for the NMDA receptor was determined by binding assays using the specific radioligand [3H] (2SR,4RS)-4-(phosphonomethyl)piperidine-2-carboxylic acid (CG...

journal_title：Bioorganic & medicinal chemistry

authors： el Hadri A,Maldivi P,Leclerc G,Rocher JP

更新日期：1995-09-01 00:00:00

abstract：:A series of structurally related citric acid-ciprofloxacin conjugates was synthesised to investigate the influence of the linker between citric acid and ciprofloxacin on antibacterial activities. Minimum inhibitory concentrations (MICs) were determined against a panel of reference strains and clinical isolates of bact...

journal_title：Bioorganic & medicinal chemistry

authors： Milner SJ,Snelling AM,Kerr KG,Abd-El-Aziz A,Thomas GH,Hubbard RE,Routledge A,Duhme-Klair AK

更新日期：2014-08-15 00:00:00

abstract：:A set of new muscarinic antagonists, bridged bicyclic derivatives of 2,2-diphenyl-[1,3]-dioxolan-4-ylmethyl-dimethylamine (1), was synthesized and tested to evaluate their affinity and selectivity for M(1), M(2), M(3) and M(4) receptor subtypes. The conformational constraint of 1 in a bicyclic structure, and the varia...

journal_title：Bioorganic & medicinal chemistry

authors： Piergentili A,Gentili F,Ghelfi F,Marucci G,Pigini M,Quaglia W,Giannella M

更新日期：2003-09-01 00:00:00

abstract：:Recent studies have identified 2,3-dimethoxy-8,9-methylenedioxy-11-[(2-dimethylamino)ethyl]-11H-isoquino[4,3-c]cinnolin-12-one (1a) as a novel topoisomerase I-targeting agent with potent cytotoxic activity. The effect of varied substituents at the 11-position of 2,3-dimethoxy-8,9-methylenedioxy-11H-isoquino[4,3-c]cinn...

journal_title：Bioorganic & medicinal chemistry

authors： Ruchelman AL,Singh SK,Ray A,Wu X,Yang JM,Zhou N,Liu A,Liu LF,LaVoie EJ

更新日期：2004-02-15 00:00:00

abstract：:Biphenylic compounds related to the natural products magnolol and 4'-O-methylhonokiol were synthesized, evaluated and optimized as positive allosteric modulators (PAMs) of GABA(A) receptors. The most efficacious compounds were the magnolol analog 5-ethyl-5'-hexylbiphenyl-2,2'-diol (45) and the honokiol analogs 4'-meth...

journal_title：Bioorganic & medicinal chemistry

authors： Fuchs A,Baur R,Schoeder C,Sigel E,Müller CE

更新日期：2014-12-15 00:00:00

abstract：:A series of ferrocene appended chalcone allied triazole coupled organosilatranes (FCTSa 7-FCTSa 12) were synthesised with the aim of amalgamating the pharmacological action of the constituting moieties into a single molecular scaffold. All the synthesised silatranes were well characterized by various spectroscopic tec...

journal_title：Bioorganic & medicinal chemistry

authors： Singh G,Arora A,Kalra P,Maurya IK,Ruizc CE,Estebanc MA,Sinha S,Goyal K,Sehgal R

更新日期：2019-01-01 00:00:00

abstract：:NS2B-NS3 is a serine protease of the Dengue virus considered a key target in the search for new antiviral drugs. In this study flavonoids were found to be inhibitors of NS2B-NS3 proteases of the Dengue virus serotypes 2 and 3 with IC50 values ranging from 15 to 44 μM. Agathisflavone (1) and myricetin (4) turned out to...

journal_title：Bioorganic & medicinal chemistry

authors： de Sousa LR,Wu H,Nebo L,Fernandes JB,da Silva MF,Kiefer W,Kanitz M,Bodem J,Diederich WE,Schirmeister T,Vieira PC

更新日期：2015-02-01 00:00:00

abstract：:A sensitive chemiluminescence (CL) sensor for berberine combined with flow-injection (FI) technology is described. The analytical reagents involved in the CL reaction, including luminol and potassium ferricyanide, were both immobilized on an anion-exchange resin column. While a volume of sodium phosphate was passed th...

journal_title：Bioorganic & medicinal chemistry

authors： Song Z,Zhao T,Wang L,Xiao Z

更新日期：2001-07-01 00:00:00

abstract：:Many therapeutically-relevant protein-protein interactions (PPIs) have been reported that feature a helix and helix-binding cleft at the interface. Given this, different approaches to disrupting such PPIs have been developed. While short peptides (<15 amino acids) typically do not fold into a stable helix, researchers...

journal_title：Bioorganic & medicinal chemistry

authors： Tennyson RL,Walker SN,Ikeda T,Harris RS,McNaughton BR

更新日期：2018-03-15 00:00:00

abstract：:A series of twenty seven substituted 2-(2-oxobenzo[d]oxazol-3(2H)-yl)acetamide derivatives were designed based on our earlier reported Mycobacterium tuberculosis (MTB) enoyl-acyl carrier protein reductase (InhA) lead. Compounds were evaluated for MTB InhA inhibition study, in vitro activity against drug-sensitive and ...

journal_title：Bioorganic & medicinal chemistry

authors： Pedgaonkar GS,Sridevi JP,Jeankumar VU,Saxena S,Devi PB,Renuka J,Yogeeswari P,Sriram D

更新日期：2014-11-01 00:00:00

abstract：:We report the synthesis and the functional studies of multiple crown alpha-helical peptides designed to form artificial ion channels. The approach combines the versatility of solid phase peptide synthesis, the conformational predictability of peptidic molecules, and the solution synthesis of crown ethers with engineer...

journal_title：Bioorganic & medicinal chemistry

authors： Biron E,Otis F,Meillon JC,Robitaille M,Lamothe J,Van Hove P,Cormier ME,Voyer N

更新日期：2004-03-15 00:00:00

abstract：:REV1 protein is a mutagenic DNA damage tolerance (DDT) mediator and encodes two ubiquitin-binding motifs (i.e., UBM1 and UBM2) that are essential for the DDT function. REV1 interacts with K164-monoubiquitinated PCNA (UbPCNA) in cells upon DNA-damaging stress. By using AlphaScreen assays to detect inhibition of REV1 an...

journal_title：Bioorganic & medicinal chemistry

authors： Vanarotti M,Evison BJ,Actis ML,Inoue A,McDonald ET,Shao Y,Heath RJ,Fujii N

更新日期：2018-05-15 00:00:00

abstract：:Bacterial DNA and synthetic oligodeoxynucleotides containing unmethylated CpG-motifs in a particular sequence context activate vertebrate immune cells. We examined the significance of negatively charged internucleoside linkages in the flanking sequences 5' and 3' to the CpG-motif on immunostimulatory activity. Cell pr...

journal_title：Bioorganic & medicinal chemistry

authors： Yu D,Kandimalla ER,Zhao Q,Cong Y,Agrawal S

更新日期：2001-11-01 00:00:00

abstract：:A fluorescent cyclodextrin-Tb(III) complex is successfully synthesized and can include bile salts in its hydrophobic cavities. Therefore, it can efficiently induce the secondary assembly of small bile salt primary micelles to large micelle aggregates, and the aggregation process can be easily observed by transmission ...

journal_title：Bioorganic & medicinal chemistry

authors： Liu Y,Zhang N,Chen Y,Chen GS

更新日期：2006-10-01 00:00:00

abstract：:In this paper, we describe a short synthesis of N-(phosphonoacetyl)-L-aspartate (PALA) analogues. The mono- and difluorinated thioacetamide precursors were prepared in one step from methyl (diethoxyphosphono)di- and monofluoromethyldithioacetates 8 and 11 as starting materials. Antiproliferating properties on a L1210 ...

journal_title：Bioorganic & medicinal chemistry

authors： Pfund E,Lequeux T,Masson S,Vazeux M,Cordi A,Pierre A,Serre V,Hervé G

更新日期：2005-08-15 00:00:00

abstract：:A series of 2',3'-exo-methylene carbocyclic nucleosides was synthesized as potential antiviral agents. These compounds were built on a bicyclo[3.1.0]hexane template that exhibits a rigid pseudoboat conformation and is capable of maintaining an identical conformation in solid state and in solution. The structures of th...

journal_title：Bioorganic & medicinal chemistry

authors： Bhushan RG,Vince R

更新日期：2002-07-01 00:00:00