Catechol derivatives of aminopyrazine and cell protection against UVB-induced mortality.

abstract：:A protein-cleaving catalyst highly selective for a disease-related protein can be used as a catalytic drug. As the first protein-cleaving catalyst selective for a protein substrate, a catalyst for myoglobin (Mb) was designed by attaching the Cu(II) or Co(III) complex of cyclen to a binding site searched by a combinato...

journal_title：Bioorganic & medicinal chemistry

authors： Jeon JW,Son SJ,Yoo CE,Hong IS,Suh J

更新日期：2003-07-03 00:00:00

abstract：:This paper describes and illustrates the use of ensemble-based docking, i.e., using a collection of protein structures in docking calculations for hit discovery, the exploration of biochemical pathways and toxicity prediction of drug candidates. We describe the computational engineering work necessary to enable large ...

journal_title：Bioorganic & medicinal chemistry

authors： Evangelista W,Weir RL,Ellingson SR,Harris JB,Kapoor K,Smith JC,Baudry J

更新日期：2016-10-15 00:00:00

abstract：:The biochemically unique structures of sugar residues in the outer cell wall of Mycobacterium tuberculosis (MTB) make the pathways for their biosynthesis and utilization attractive targets for the development of new and selective anti-tubercular agents. A cell-free assay system for galactosyltransferase activity using...

journal_title：Bioorganic & medicinal chemistry

authors： Pathak AK,Besra GS,Crick D,Maddry JA,Morehouse CB,Suling WJ,Reynolds RC

更新日期：1999-11-01 00:00:00

abstract：:This study describes the synthesis and radiosynthesis of eight new [18F]fluoro-inositol-based radiotracers in myo- and scyllo-inositol configuration. These radiotracers are equipped with a propyl linker bearing fluorine-18. This fluorinated arm is either on a hydroxyl group, i.e. O-alkylated inositols, or on the cyclo...

journal_title：Bioorganic & medicinal chemistry

authors： Collet C,Schmitt S,Maskali F,Clément A,Chrétien F,Karcher G,Marie PY,Poussier S,Lamandé-Langle S

更新日期：2017-10-15 00:00:00

abstract：:In order to develop structure-activity relationships and to provide access to antibacterial agents for dual action studies, a variety of aryl group-substituted 2-aryl-5-nitro-1H-indoles were synthesized and the activity of the compounds assessed as inhibitors of the NorA multidrug resistance pump in the bacterium Stap...

journal_title：Bioorganic & medicinal chemistry

authors： Samosorn S,Bremner JB,Ball A,Lewis K

更新日期：2006-02-01 00:00:00

abstract：:A library of chalcones with basic functionalities were screened for inhibition of P-glycoprotein (Pgp, ABCB1) by the calcein-AM accumulation assay on MDCKII/MDR1 cells. Three members that had ring A substituted with 5-(1-ethylpiperidin-4-yl) and 2,4-dimethoxy groups were found to increase calcein-AM accumulation to a ...

journal_title：Bioorganic & medicinal chemistry

authors： Liu XL,Tee HW,Go ML

更新日期：2008-01-01 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：:1,2,3-Triazole-, arylamino- and thio-substituted naphthoquinones (24, 8, and 2 representatives, respectively) were synthesized in moderate yields and evaluated against several human cancer cell lines (blood, ovarian, breast, central nervous system, colon, and prostate cancers and melanoma), showing, for some of them, ...

journal_title：Bioorganic & medicinal chemistry

authors： da Cruz EH,Hussene CM,Dias GG,Diogo EB,de Melo IM,Rodrigues BL,da Silva MG,Valença WO,Camara CA,de Oliveira RN,de Paiva YG,Goulart MO,Cavalcanti BC,Pessoa C,da Silva Júnior EN

更新日期：2014-03-01 00:00:00

abstract：:The preparation of novel 5-aryl-2-thio-1,3,4-oxadiazoles 4a-41 and the computer-aided study of their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv (ATCC 27294) are reported. The average accuracy of the electronic-topological method and neural network methods applied to the activity predict...

journal_title：Bioorganic & medicinal chemistry

authors： Macaev F,Rusu G,Pogrebnoi S,Gudima A,Stingaci E,Vlad L,Shvets N,Kandemirli F,Dimoglo A,Reynolds R

更新日期：2005-08-15 00:00:00

abstract：:The effect of various natural flavonoids, cinnamic acid derivatives, and a series of synthetic flavones on cell proliferation was evaluated in vitro in a panel of established human and murine tumor cell lines. The most potent antiproliferative agents were caffeic acid n-butyl ester (12) > 2'-nitroflavone (26) > caffei...

journal_title：Bioorganic & medicinal chemistry

authors： Cárdenas M,Marder M,Blank VC,Roguin LP

更新日期：2006-05-01 00:00:00

abstract：:In previous studies, the polycyclic cage amine 8-benzylamino-8,11-oxapentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]undecane (NGP1-01) and a number of its derivatives showed positive effects in neuroprotection studies with MPTP, in vivo. In view of these findings, we examined these compounds for their effects on [(3)H]dopamin...

journal_title：Bioorganic & medicinal chemistry

authors： Geldenhuys WJ,Malan SF,Murugesan T,Van der Schyf CJ,Bloomquist JR

更新日期：2004-04-01 00:00:00

abstract：:Metabotropic glutamate receptor 5 (mGlu5) is a biological target implicated in major neurological and psychiatric disorders. In the present study, we have investigated structural determinants of the interaction of negative allosteric modulators (NAMs) with the seven-transmembrane (7TM) domain of mGlu5. A homology mode...

journal_title：Bioorganic & medicinal chemistry

authors： Anighoro A,Graziani D,Bettinelli I,Cilia A,De Toma C,Longhi M,Mangiarotti F,Menegon S,Pirona L,Poggesi E,Riva C,Rastelli G

更新日期：2015-07-01 00:00:00

abstract：:Synthesis and antitumor activity of goniofufurone analogues 15, 16, 17, 33, and 46 is reported. Key step in the synthesis is Pd (II) mediated oxidative cyclisation of vinyl-(hydroxy) furans 18, 19 to the corresponding lactols 32, 43. Cytotoxicities of 15, 16, 17, 33, and 46 tested against six human cancer cell lines a...

journal_title：Bioorganic & medicinal chemistry

authors： Mereyala HB,Gadikota RR,Joe M,Arora SK,Dastidar SG,Agarwal S

更新日期：1999-09-01 00:00:00

abstract：:We efficiently synthesized 2'-O,4'-C-aminomethylene-bridged nucleic acid (2',4'-BNANC) monomers bearing the four nucleobases, guanine, adenine, thymine, and 5-methylcytosine and incorporated these monomers into oligonucleotides. Initially, we carried out the transglycosylation reaction on several 2'-O-substituted 5-me...

journal_title：Bioorganic & medicinal chemistry

authors： Fujisaka A,Hari Y,Takuma H,Rahman SMA,Yoshikawa H,Pang J,Imanishi T,Obika S

更新日期：2019-04-15 00:00:00

abstract：:Recent studies have focused on prostaglandin E₂ (PGE₂) because PGE₂ regulates vertebrate hematopoietic stem cell induction and engraftment. PGE₂ acts through EP2 and EP4 receptors to mediate regeneration and hematopoietic stem cell (HSC) development via the Wnt signaling pathway. Previously we reported that inhibitors...

journal_title：Bioorganic & medicinal chemistry

authors： Piao YL,Ram Song A,Cho H

更新日期：2015-05-01 00:00:00

abstract：:As HIV-associated dementia prevalence has risen with the lifespan of HIV-infected individuals, there is an important need for antiretroviral and anti-inflammatory drugs targeting the central nervous system. Platelet-activating factor, a mediator of inflammation, is an HIV-induced neurotoxin secreted in the infected br...

journal_title：Bioorganic & medicinal chemistry

authors： Sallem W,Serradji N,Dereuddre-Bosquet N,Dive G,Clayette P,Heymans F

更新日期：2006-12-01 00:00:00

abstract：:Amyloid-β (Aβ) and tau protein are two crucial hallmarks in Alzheimer's disease (AD). Their aggregation forms are thought to be toxic to the neurons in the brain. A series of new 1,2,3,4-tetrahydro-1-acridone analogues were designed, synthesized, and evaluated as potential dual inhibitors for Aβ and tau aggregation. I...

journal_title：Bioorganic & medicinal chemistry

authors： Lv P,Xia CL,Wang N,Liu ZQ,Huang ZS,Huang SL

更新日期：2018-09-01 00:00:00

abstract：:6-N-(Benzothiazol-2-yl)deoxyadenosine (A(BT)) was synthesized and incorporated into DNAs. Although, the multipoint benzothiazole (BT) modification of oligodeoxynucleotides reduced the stability of duplexes with their complementary strands, it induced the strong exciton coupling between BT moieties. The circular dichro...

journal_title：Bioorganic & medicinal chemistry

authors： Masaki Y,Ohkubo A,Seio K,Sekine M

更新日期：2010-01-15 00:00:00

abstract：:The anti-inflammatory properties of a heparin-like compound from the shrimp Litopenaeus vannamei are related. Besides reducing significantly (p<0.001) the influx of inflammatory cells to injury site in a model of acute inflammation, shrimp heparin-like compound was able to reduce the matrix metalloproteinase (MMPs) ac...

journal_title：Bioorganic & medicinal chemistry

authors： Brito AS,Arimatéia DS,Souza LR,Lima MA,Santos VO,Medeiros VP,Ferreira PA,Silva RA,Ferreira CV,Justo GZ,Leite EL,Andrade GP,Oliveira FW,Nader HB,Chavante SF

更新日期：2008-11-01 00:00:00

abstract：:3-(4-Piperidinyl)-5-arylpyrazoles, such as 1, were selective for the cloned human dopamine D4 receptor (hD4), but also showed affinity at voltage sensitive calcium, sodium and potassium ion channels. A combination of substituent changes to reduce the basicity of the piperidine nitrogen and conformational restriction t...

journal_title：Bioorganic & medicinal chemistry

authors： Collins I,Rowley M,Davey WB,Emms F,Marwood R,Patel S,Patel S,Fletcher A,Ragan IC,Leeson PD,Scott AL,Broten T

更新日期：1998-06-01 00:00:00

abstract：:The preserved fungal species Antrodia camphorata has diverse health-promoting effects and has been popularly used in East Asia as a traditional herb. We isolated a volatile compound from the culture medium of A. camphorata and identified it as gamma-dodecalactone (gamma-DDL). Cytomic screening for immune-modulating ac...

journal_title：Bioorganic & medicinal chemistry

authors： Chen CJ,Vijaya Krishna R,Tsai CC,Wu WH,Chao LK,Hwang KH,Chien CM,Chang HY,Chen ST

更新日期：2010-09-15 00:00:00

abstract：:A number of N-substituted 2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles were synthesized and evaluated for their antiproliferative activities. The panel substitution included alkyl, aryl, and morpholinoalkyl derivatives. The structures of compounds were identified from elemental, IR, (1)H NMR, (13)C NMR and MS sp...

journal_title：Bioorganic & medicinal chemistry

authors： Matysiak J,Opolski A

更新日期：2006-07-01 00:00:00

abstract：:Streptococcus pneumoniae is among the major human pathogens. Several interactions of this bacterium with its host appear to have been mediated by bacterial cell wall components. Specifically, phosphorylcholine residues covalently attached to teichoic and lipoteichoic acids serve as anchors for many surface-located pro...

journal_title：Bioorganic & medicinal chemistry

authors： Campillo NE,Páez JA,Lagartera L,Gonzalez A

更新日期：2005-12-01 00:00:00

abstract：:A series of triaminotriazine derivatives (compounds 5a-f, 6a-x, and 7a-g) was designed, synthesized, and evaluated for their inhibition activities to colorectal cancer (CRC) cell lines (HCT-116 and HT-29). Most of the synthesized compounds demonstrated moderate anti-proliferatory effects on both HCT-116 and HT-29 cell...

journal_title：Bioorganic & medicinal chemistry

authors： Zheng M,Xu C,Ma J,Sun Y,Du F,Liu H,Lin L,Li C,Ding J,Chen K,Jiang H

更新日期：2007-02-15 00:00:00

abstract：:In this Letter, we investigated the binding properties towards nucleic acids of a thymine-functionalized oligolysine, composed of nucleobase-bearing amino acid moieties and underivatized l-lysine residues alternate in the backbone. The basic nucleopeptide proved to be well soluble in water and able to interact with bo...

journal_title：Bioorganic & medicinal chemistry

authors： Roviello GN,Musumeci D,D'Alessandro C,Pedone C

更新日期：2014-02-01 00:00:00

abstract：:A series of Celecoxib analogues or derivatives were designed and synthesized, and their biological activities were studied. The results of inhibitory activity in vitro proved that compounds 1a, 1h, 1i, 1l and 1p had better inhibitory effect on COX-2, and the selectivity was higher. Among them, the inhibitory activity ...

journal_title：Bioorganic & medicinal chemistry

authors： Zhou S,Yang S,Huang G

更新日期：2017-09-01 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

abstract：:Iron complexes (1-7) involving N6-benzyladenosine derivatives of the predominant composition [Fe(L(n))Cl(3)].H(2)O {where L(1)=N6-(2-fluorobenzyl)adenosine (1), L(2)=N6-(4-fluorobenzyl)adenosine (2), L(3)=N6-(2-trifluoromethylbenzyl)adenosine (3), L(4)=N6-(3-trifluoromethylbenzyl)adenosine (4), L(5)=N6-(4-trifluoromet...

journal_title：Bioorganic & medicinal chemistry

authors： Trávnícek Z,Mikulík J,Cajan M,Zboril R,Popa I

更新日期：2008-09-15 00:00:00

abstract：:Fibroblast grow factor receptor 1 (FGFR1) is an important anti-cancer target that plays crucial role in oncogenesis and oncogenic angiogenesis. The structure-activity relationship (SAR) of N-phenylthieno[2,3-d]pyrimidin-4-amines was investigated. Binding of active compounds with FGFR1 kinase was analyzed by molecular ...

journal_title：Bioorganic & medicinal chemistry

authors： Gryshchenko AA,Bdzhola VG,Balanda AO,Briukhovetska NV,Kotey IM,Golub AG,Ruban TP,Lukash LL,Yarmoluk SM

更新日期：2015-05-01 00:00:00

abstract：:Four kinds of tetravalent double-headed glycoclusters [(LacNAc)4-DHGs] were designed with linkers of varying lengths consisting of alkanedioic carboxyamido groups (C6, C12, C18 and C24) between two bi-antennary LacNAc-glycosides. These glycoclusters served as high-affinity cross-linking ligands for the LacNAc-binding ...

journal_title：Bioorganic & medicinal chemistry

authors： Ogata M,Chuma Y,Yasumoto Y,Onoda T,Umemura M,Usui T,Park EY

更新日期：2016-01-01 00:00:00