Design of a pyrene-containing fluorescence probe for labeling of RNA poly(A) tracts.


:A labeling probe containing a pyrenecarboxamide-tethered modified DNA base, (Py)U, has been developed for fluorometric detection of RNA poly(A) tracts, in which the fluorescence emission intensity was controlled by the microstructural change around (Py)U caused by binding with the target RNA.


Bioorg Med Chem


Tanaka K,Okamoto A




Has Abstract


2008-01-01 00:00:00














  • Synthesis and biological evaluation of 1,4-dihydropyridine calcium channel modulators having a diazen-1-ium-1,2-diolate nitric oxide donor moiety for the potential treatment of congestive heart failure.

    abstract::A group of racemic 4-aryl(heteroaryl)-1,4-dihydro-2,6-dimethyl-3-nitropyridines possessing nitric oxide donor O(2)-acetoxymethyl-1-(N-ethyl-N-methylamino, or 4-ethylpiperazin-1-yl)diazen-1-ium-1,2-diolate, C-5 ester substituents were synthesized by coupling the respective 4-aryl(heteroaryl)-1,4-dihydro-2,6-dimethyl-3-...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Velázquez C,Knaus EE

    更新日期:2004-07-15 00:00:00

  • Probing the general time scale question of boronic acid binding with sugars in aqueous solution at physiological pH.

    abstract::The boronic acid group is widely used in chemosensor design due to its ability to reversibly bind diol-containing compounds. The thermodynamic properties of the boronic acid-diol binding process have been investigated extensively. However, there are few studies of the kinetic properties of such binding processes. In t...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Ni N,Laughlin S,Wang Y,Feng Y,Zheng Y,Wang B

    更新日期:2012-05-01 00:00:00

  • Cytotoxic heterocyclic triterpenoids derived from betulin and betulinic acid.

    abstract::The aim of this work was to synthesize a set of heterocyclic derivatives of lupane, lup-20(29)-ene, and 18α-oleanane, and to investigate their cytotoxic activities. Some of those heterocycles were previously known in the oleanane (allobetulin) group; however, to our knowledge the syntheses and biological activities of...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Urban M,Vlk M,Dzubak P,Hajduch M,Sarek J

    更新日期:2012-06-01 00:00:00

  • 2-N-Methyl modifications and SAR studies of manzamine A.

    abstract::Quaternary carbolinium salts have been reported to show improved antimalarial activity and reduced cytotoxicity as compared to electronically neutral beta-carbolines. In this study, mono- and di-methylated quaternary carbolinium cations of manzamine A were synthesized and evaluated for their in vitro antimalarial and ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Ibrahim MA,Shilabin AG,Prasanna S,Jacob M,Khan SI,Doerksen RJ,Hamann MT

    更新日期:2008-07-15 00:00:00

  • Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors.

    abstract::A new series of selective PDE4D inhibitors has been designed and synthesized by replacing 3-methoxy group with 3-difluoromethoxy isoster moiety in our previously reported cathecolic structures. All compounds showed a good PDE4D3 inhibitory activity, most of them being inactive toward other PDE4 isoforms (PDE4A4, PDE4B...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Brullo C,Massa M,Villa C,Ricciarelli R,Rivera D,Pronzato MA,Fedele E,Barocelli E,Bertoni S,Flammini L,Bruno O

    更新日期:2015-07-01 00:00:00

  • Carbonic anhydrases as targets for medicinal chemistry.

    abstract::Carbonic anhydrases (CAs, EC are zinc enzymes acting as efficient catalysts for the reversible hydration of carbon dioxide to bicarbonate. 16 different alpha-CA isoforms were isolated in mammals, where they play crucial physiological roles. Some of them are cytosolic (CA I, CA II, CA III, CA VII, CA XIII), ot...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章,评审


    authors: Supuran CT,Scozzafava A

    更新日期:2007-07-01 00:00:00

  • Comparison of the dark and light-induced toxicity of thio and seleno analogues of the thiopyrylium dye AA1.

    abstract::2,6-Bis(4-anilino)-4-(4-N,N-dimethylanilino)thiopyrylium chloride (AA1) and -selenopyrylium chloride (AA1-Se) and 2,6-bis(4-anilino)-4-(4-N-morpholinophenyl)thiopyrylium chloride (1) and -selenopyrylium chloride (2) were prepared via the addition of 4-N,N-dimethylanilino magnesium bromide and 4-N-morpholinophenyl magn...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Detty MR,Gibson SL,Hilf R

    更新日期:2004-05-15 00:00:00

  • Synthesis, structure, and antimycobacterial activity of 6-[1(3H)-isobenzofuranylidenemethyl]purines and analogs.

    abstract::6-Benzofuryl-, styryl, benzyl, and furfurylpurines as well as 6-[1(3H)-isobenzofuranylidenemethyl]purines have been synthesized and their activities against Mycobacterium tuberculosis (Mtb) determined. Several compounds displayed profound antimycobacterial activity in combination with low toxicity towards mammalian ce...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Braendvang M,Bakken V,Gundersen LL

    更新日期:2009-09-15 00:00:00

  • Synthesis and biological relationships of 3',6-substituted 2-phenyl-4-quinolone-3-carboxylic acid derivatives as antimitotic agents.

    abstract::As part of a continuing search for potential anticancer drug candidates in the 2-phenyl-4-quinolone series, 3',6-substituted 2-phenyl-4-quinolone-3-carboxylic acid derivatives and their salts were synthesized and evaluated. Preliminary screening showed that carboxylic acid analogs containing a m-fluoro substituted 2-p...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Lai YY,Huang LJ,Lee KH,Xiao Z,Bastow KF,Yamori T,Kuo SC

    更新日期:2005-01-03 00:00:00

  • New potent antibacterials against Gram-positive multiresistant pathogens: effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles.

    abstract::The effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles have been studied to design new potent antibacterials against Gram-positive multidrug-resistant pathogens. The adopted strategy involved a molecular modelling approach, the synthesis and biological evaluation of new designed compo...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Fortuna CG,Berardozzi R,Bonaccorso C,Caltabiano G,Di Bari L,Goracci L,Guarcello A,Pace A,Palumbo Piccionello A,Pescitelli G,Pierro P,Lonati E,Bulbarelli A,Cocuzza CE,Musumarra G,Musumeci R

    更新日期:2014-12-15 00:00:00

  • Polymer supported synthesis of a natural product-inspired oxepane library.

    abstract::Natural product inspired compound collections are prevalidated due to the evolutionary selection of the natural product scaffolds. Their synthesis requires the development of novel strategies amenable to formats suitable for library build-up. We describe a method for the synthesis of an oxepane library inspired by the...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Basu S,Waldmann H

    更新日期:2014-08-15 00:00:00

  • New cannabinoid receptor antagonists as pharmacological tool.

    abstract::Synthesis and pharmacological evaluation of a new series of cannabinoid receptor antagonists of indazole ether derivatives have been performed. Pharmacological evaluation includes radioligand binding assays with [3H]-CP55940 for CB1 and CB2 receptors and functional activity for cannabinoid receptors on isolated tissue...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: González-Naranjo P,Pérez C,Girón R,Sánchez-Robles EM,Martín-Fontelles MI,Carrillo-López N,Martín-Vírgala J,Naves M,Campillo NE,Páez JA

    更新日期:2020-10-01 00:00:00

  • Anti-AIDS agents--XIX. Neotripterifordin, a novel anti-HIV principle from Tripterygium wilfordii: isolation and structural elucidation.

    abstract::A new kaurane type diterpene lactone, neotripterifordin (1), has been isolated from the roots of Tripterygium wilfordii. The structure of 1 was elucidated by spectroscopic methods, which included the concerted application of a number of 2-D NMR techniques including 1H-1H COSY, phase-sensitive NOESY, HETCOR, and long-r...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Chen K,Shi Q,Fujioka T,Nakano T,Hu CQ,Jin JQ,Kilkuskie RE,Lee KH

    更新日期:1995-10-01 00:00:00

  • Synthesis and biological evaluation of 4,5-dihydro-1H-pyrazole derivatives as potential nNOS/iNOS selective inhibitors. Part 2: Influence of diverse substituents in both the phenyl moiety and the acyl group.

    abstract::In a preliminary article, we reported a series of 4,5-dihydro-1H-pyrazole derivatives as neuronal nitric oxide synthase (nNOS) inhibitors. Here we present the data about the inhibition of inducible nitric oxide synthase (iNOS) of these compounds. In general, we can confirm that these pyrazoles are nNOS selective inhib...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Carrión MD,Chayah M,Entrena A,López A,Gallo MA,Acuña-Castroviejo D,Camacho ME

    更新日期:2013-07-15 00:00:00

  • Induction of enantio-selective apoptosis in human leukemia HL-60 cells by (S)-erypoegin K, an isoflavone isolated from Erythrina poeppigiana.

    abstract::Erypoegin K, an isoflavone isolated from the stem bark of Erythrina poeppigiana, has potent apoptosis-inducing effect on human leukemia HL-60 cells. Erypoegin K has a chiral carbon at the C-2'' position of its furan ring and naturally occurs as a racemic mixture of (S)- and (R)-isomers. In the present study, we semi-s...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Hikita K,Saigusa S,Takeuchi Y,Matsuyama H,Nagai R,Kato K,Murata T,Tanaka H,Wagh YS,Asao N,Kaneda N

    更新日期:2020-06-01 00:00:00

  • A-ring and E-ring modifications of the cytotoxic alkaloid Luotonin A: Synthesis, computational and biological studies.

    abstract::A series of new Luotonin A derivatives with substituents at rings A and E was synthesized, together with some E-ring-unsubstituted derivatives. Subsequently, the compound library was examined in silico for their binding into a previously proposed site in the DNA/topoisomerase I binary complex. Whereas no convincing co...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Ibric A,Battisti V,Deckardt S,Haller AV,Lee C,Prötsch C,Langer T,Heffeter P,Schueffl HH,Marian B,Haider N

    更新日期:2020-05-01 00:00:00

  • Immunostimulatory activity of CpG oligonucleotides containing non-ionic methylphosphonate linkages.

    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

    pub_type: 杂志文章


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

    更新日期:2001-11-01 00:00:00

  • Syntheses and evaluation of antioxidant activity of sydnonyl substituted thiazolidinone and thiazoline derivatives.

    abstract::3-Aryl-4-formylsydnone 4'-phenylthiosemicarbazones (3a-d) and 3-aryl-4-formylsydnone thiosemicarbazones (3e-h), which are precursors of 3-aryl-4-heterocyclic sydnones, are prepared by the condensation of 3-aryl-4-formylsydnones (1a-d) with 4'-phenylthiosemicarbazide (2a) and thiosemicarbazide (2b), respectively. The t...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Shih MH,Ke FY

    更新日期:2004-09-01 00:00:00

  • Study on synthesis, characterization and biological activity of some new nitrogen heterocycle porphyrins.

    abstract::Seven new nitrogen heterocycle porphyrins, 5,10,15,20-tetra[4-(N-pyrrolidinyl)phenyl]porphine (TBPPH(2)), 5,10,15,20-tetra[4-(4'-ethylpiperazinyl)phenyl]porphine (TEPPH(2)), 5,10,15,20-tetra [4-(4'-butylpiperazinyl)phenyl]porphine (TUPPH(2)), 5,10,15,20-tetra[4-(4'-heptylpiperazinyl) phenyl]porphine (THPPH(2)), 5-[4-(...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Guo CC,Li HP,Zhang XB

    更新日期:2003-04-17 00:00:00

  • Syntheses and pharmacological characterization of novel thiazole derivatives as potential mGluR5 PET ligands.

    abstract::Four novel thiazole containing ABP688 derivatives were synthesized and evaluated for their binding affinity towards the metabotropic glutamate receptor subtype 5 (mGluR5). (E)-3-((2-(Fluoromethyl)thiazol-4-yl)ethynyl)cyclohex-2-enone O-methyl oxime (FTECMO), the ligand with the highest binding affinity (K(i)=5.5+/-1.1...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Baumann CA,Mu L,Wertli N,Krämer SD,Honer M,Schubiger PA,Ametamey SM

    更新日期:2010-08-15 00:00:00

  • Discovery and development of DNA polymerase IIIC inhibitors to treat Gram-positive infections.

    abstract::Despite the growing global crisis caused by antimicrobial drug resistance among pathogenic bacteria, the number of new antibiotics, especially new chemical class of antibiotics under development is insufficient to tackle the problem. Our review focuses on an emerging class of antibacterial therapeutic agents that hold...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章,评审


    authors: Xu WC,Silverman MH,Yu XY,Wright G,Brown N

    更新日期:2019-08-01 00:00:00

  • Preparation, antimicrobial evaluation, and mutagenicity of [2-hydroxyaryl]-[1-methyl-5-nitro-1H-2-imidazolyl]methanols , [5-tert-butyl-2-methylaminophenyl]-[1-methyl-5-nitro-1H-2-imidazo lyl]me thanol, and [2-hydroxyaryl]-[1-methyl-5-nitro-1H-2-imidazolyl

    abstract::Efficient preparations of the titled compounds are described, their antimicrobial activity and mutagenic properties being evaluated. Some of the studied compounds are nonmutagenic and present a MIC as low as some of the usual standards in the field. ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Arredondo Y,Moreno-Mañas M,Pleixats R,Palacín C,Raga MM,Castelló JM,Ortiz JA

    更新日期:1997-10-01 00:00:00

  • Synthesis and characterization of mitoQ and idebenone analogues as mediators of oxygen consumption in mitochondria.

    abstract::Analogues of mitoQ and idebenone were synthesized to define the structural elements that support oxygen consumption in the mitochondrial respiratory chain. Eight analogues were prepared and fully characterized, then evaluated for their ability to support oxygen consumption in the mitochondrial respiratory chain. While...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Duveau DY,Arce PM,Schoenfeld RA,Raghav N,Cortopassi GA,Hecht SM

    更新日期:2010-09-01 00:00:00

  • Biology-oriented synthesis of benzopyrano[3,4-c]pyrrolidines.

    abstract::A natural product inspired synthesis of 6,6,5-tricyclic compounds via a silver(I)-catalyzed formal 1,3-dipolar cycloaddition of coumarins with α-iminoesters was developed. The reaction proceeds in a stepwise reaction course under formation of the trans-substituted diastereomer with respect to the 1,3-dipole and shows ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Potowski M,Golz C,Strohmann C,Antonchick AP,Waldmann H

    更新日期:2015-06-15 00:00:00

  • Structure-based design and synthesis of small molecule protein-tyrosine phosphatase 1B inhibitors.

    abstract::Protein-tyrosine phosphatase (PTP) inhibitors are attractive as potential signal transduction-directed therapeutics which may be useful in the treatment of a variety of diseases. We have previously reported the X-ray structure of 1,1-difluoro-1-(2-naphthalenyl)methyl] phosphonic acid (4) complexed with the human the p...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Yao ZJ,Ye B,Wu XW,Wang S,Wu L,Zhang ZY,Burke TR Jr

    更新日期:1998-10-01 00:00:00

  • Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylase based on a cinnamic hydroxamic acid core structure.

    abstract::Small molecules that act on multiple biological targets have been proposed to combat the drug resistance commonly observed for cancer chemotherapy. By combining the structural features of known inhibitors of inosine monophosphate dehydrogense (IMPDH) and histone deacetylase (HDAC), dual inhibitors of IMPDH and HDAC ba...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Chen L,Petrelli R,Gao G,Wilson DJ,McLean GT,Jayaram HN,Sham YY,Pankiewicz KW

    更新日期:2010-08-15 00:00:00

  • NMR determination of Electrophorus electricus acetylcholinesterase inhibition and reactivation by neutral oximes.

    abstract::Neurotoxic organophosphorus compounds (OPs), which are used as pesticides and chemical warfare agents lead to more than 700,000 intoxications worldwide every year. The main target of OPs is the inhibition of acetylcholinesterase (AChE), an enzyme necessary for the control of the neurotransmitter acetylcholine (ACh). T...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: da Cunha Xavier Soares SF,Vieira AA,Delfino RT,Figueroa-Villar JD

    更新日期:2013-09-15 00:00:00

  • N-substituted homopiperazine barbiturates as gelatinase inhibitors.

    abstract::Matrix metalloproteinases are implicated in a wide range of pathophysiological processes and potent selective inhibitors for these enzymes continue to be eagerly sought. 5,5-Disubstituted barbiturates hold promise as inhibitor types being stable in vivo and relatively selective for the gelatinases (MMP-2 and MMP-9). I...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Wang J,Medina C,Radomski MW,Gilmer JF

    更新日期:2011-08-15 00:00:00

  • Doxifluridine-conjugated 2-5A analog shows strong RNase L activation ability and tumor suppressive effect.

    abstract::RNase L is activated by 2',5'-oligoadenylates (2-5A) at subnanomolar levels to cleave single-stranded RNA. We previously reported the hypothesis that the introduction of an 8-methyladenosine residue at the 2'-terminus of the 2-5A tetramer shifts the 2-5A binding site of RNase L. In this study, we synthesized various 5...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Kitamura Y,Kito S,Nakashima R,Tanaka K,Nagaoka K,Kitade Y

    更新日期:2016-08-15 00:00:00

  • Synthesis, structure, molecular docking, and structure-activity relationship analysis of enamines: 3-aryl-4-alkylaminofuran-2(5H)-ones as potential antibacterials.

    abstract::Thirty-one 3-aryl-4-alkylaminofuran-2(5H)-ones were designed, prepared and tested for their antibacterial activity. Some of them showed significant antibacterial activity against Gram-positive organisms, especially against Staphylococcus aureus ATCC 25923, but all were inactive against Gram-negative organisms. Out of ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Xiao ZP,He XB,Peng ZY,Xiong TJ,Peng J,Chen LH,Zhu HL

    更新日期:2011-03-01 00:00:00