Development of polymeric drug delivery system for recognizing vascular endothelial dysfunction.


:The vascular endothelium plays an important role in regulating vascular homeostasis. Damage to the endothelium can lead to cardiovascular diseases such as arteriosclerosis. Therefore, early-stage detection and evaluation of vascular endothelium dysfunction would be very important for effective diagnosis and therapy. We synthesized a polymeric drug carrier bearing an Evans blue analogue as a probing unit for endothelium injury. The polymeric carrier spontaneously formed stable nanoparticles with micelle-like structure in aqueous media and could encapsulate hydrophobic doxorubicin (DOX). The encapsulated DOX showed a sustainable release profile over a period of 10-60 h depending on the loaded DOX concentration. The polymeric carrier specifically adsorbed against the endothelium-injured site in extracted porcine aorta. These properties of the polymeric drug carrier will be suitable for specific drug delivery to endothelium dysfunctional region.


Bioorg Med Chem


Ikuta K,Mori T,Yamamoto T,Niidome T,Shimokawa H,Katayama Y




Has Abstract


2008-03-15 00:00:00














  • Conjugation of a 3-(1H-phenanthro[9,10-d]imidazol-2-yl)-1H-indole intercalator to a triplex oligonucleotide and to a three-way junction.

    abstract::A new intercalating nucleic acid monomer M comprising a 4-(1-indole)-butane-1,2-diol moiety was synthesized via a classical alkylation reaction of indole-3-carboxaldehyde followed by a condensation reaction with phenanthrene-9,10-dione in the presence of ammonium acetate to form a phenanthroimidazole moiety linked to ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Fatthalla MI,Elkholy YM,Abbas NS,Mandour AH,Jørgensen PT,Bomholt N,Pedersen EB

    更新日期:2012-01-01 00:00:00

  • Chemical and microbial semi-synthesis of tetrahydroprotoberberines as inhibitors on tissue factor procoagulant activity.

    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

    pub_type: 杂志文章


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

    更新日期:2013-01-01 00:00:00

  • Nicorandil analogues containing NO-donor furoxans and related furazans.

    abstract::The synthesis and in vitro vasodilating properties of hybrid compounds in which furoxan (1,2,5-oxadiazole 2-oxide) moieties, endowed with different NO-donor properties, were substituted for the nitroxy function of Nicorandil are reported. The corresponding cyanoguanidine analogues are also considered. This approach ha...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Boschi D,Cena C,Di Stilo A,Fruttero R,Gasco A

    更新日期:2000-07-01 00:00:00

  • Design, synthesis, conformational analysis, and biological studies of urotensin-II lactam analogues.

    abstract::Human urotensin II (hU-II; H-Glu-Thr-Pro-Asp-cyclo[Cys-Phe-Trp-Lys-Tyr-Cys]-Val-OH) is a disulfide bridged undecapeptide recently identified as the ligand of an orphan G protein-coupled receptor. hU-II has been described as the most potent vasoconstrictor compound identified to date. With the aim of replacing the disu...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Grieco P,Carotenuto A,Patacchini R,Maggi CA,Novellino E,Rovero P

    更新日期:2002-12-01 00:00:00

  • Synthesis and insecticidal activity studies of novel phenylpyrazole derivatives containing arylimine or carbimidate moiety.

    abstract::Phenylpyrazole insecticides are successful for crop protection and public hygiene by blocking gamma-aminobutyric acid (GABA)-gated chloride channels and glutamate-gated chloride (GluCl) channels. A series of novel phenylpyrazoles containing arylimine or 1-methoxyaryl groups were designed and synthesized. The addition ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Zhao Q,Sun R,Liu Y,Chen P,Li Y,Yang S,Wang Q

    更新日期:2019-11-01 00:00:00

  • A new structural alternative in benzo[b]furans for antimicrobial activity.

    abstract::Two series of 2-substituted and three new diacetyl benzofurans were synthesized through palladium-catalyzed reactions and their in vitro antimicrobial spectra were assessed. The compounds demonstrated mild to significant growth inhibition against antibiotic-susceptible standard and clinically isolated strains of Gram-...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Wahab Khan M,Jahangir Alam M,Rashid MA,Chowdhury R

    更新日期:2005-08-15 00:00:00

  • Active site mapping of trypsin, thrombin and matriptase-2 by sulfamoyl benzamidines.

    abstract::The benzamidine moiety, a well-known arginine mimetic, has been introduced in a variety of ligands, including peptidomimetic inhibitors of trypsin-like serine proteases. According to their primary substrate specificity, the benzamidine residue interacts with the negatively charged aspartate at the bottom of the S1 poc...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Dosa S,Stirnberg M,Lülsdorff V,Häußler D,Maurer E,Gütschow M

    更新日期:2012-11-01 00:00:00

  • Synthesis of both enantiomers of hydroxypipecolic acid derivatives equivalent to 5-azapyranuronic acids and evaluation of their inhibitory activities against glycosidases.

    abstract::We have synthesized 3-hydroxy- and 3,4,5-trihydroxypipecolic acid derivatives corresponding to 5-aza derivatives of uronic acids and evaluated their inhibitory activities against various glycosidases including beta-glucuronidase. Compounds 4 and 5 were chosen as common intermediates for the synthesis of 3,4,5-trihydro...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Yoshimura Y,Ohara C,Imahori T,Saito Y,Kato A,Miyauchi S,Adachi I,Takahata H

    更新日期:2008-09-01 00:00:00

  • Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds.

    abstract::A set of 116 structurally very diverse compounds, mainly drugs, was characterized by 1630 molecular descriptors. The biological property modelled in this study was the transdermal permeability coefficient logK(p). The main objective was to find a limited set of suitable model compounds for skin penetration studies. Th...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Baert B,Deconinck E,Van Gele M,Slodicka M,Stoppie P,Bodé S,Slegers G,Vander Heyden Y,Lambert J,Beetens J,De Spiegeleer B

    更新日期:2007-11-15 00:00:00

  • Rickettsia prowazekii methionine aminopeptidase as a promising target for the development of antibacterial agents.

    abstract::Methionine aminopeptidase (MetAP) is a class of ubiquitous enzymes essential for the survival of numerous bacterial species. These enzymes are responsible for the cleavage of N-terminal formyl-methionine initiators from nascent proteins to initiate post-translational modifications that are often essential to proper pr...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Helgren TR,Chen C,Wangtrakuldee P,Edwards TE,Staker BL,Abendroth J,Sankaran B,Housley NA,Myler PJ,Audia JP,Horn JR,Hagen TJ

    更新日期:2017-02-01 00:00:00

  • Exogenous fluorescent tracer agents based on pegylated pyrazine dyes for real-time point-of-care measurement of glomerular filtration rate.

    abstract::Novel pyrazine carboxamides bearing hydrophilic poly(ethylene glycol) (PEG) moieties were designed, synthesized, and evaluated for use as fluorescent glomerular filtration rate (GFR) tracer agents. Among these, compounds 4d and 5c that contain about 48 ethylene oxide units in the PEG chain exhibited the most favorable...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Poreddy AR,Neumann WL,Freskos JN,Rajagopalan R,Asmelash B,Gaston KR,Fitch RM,Galen KP,Shieh JJ,Dorshow RB

    更新日期:2012-04-15 00:00:00

  • Conformationally locked thiosugars as potent alpha-mannosidase inhibitors: synthesis, biochemical and docking studies.

    abstract::A series of thiosugar derivatives (thiolevomannosans) derived from mannose were synthesized and their inhibitory activity was tested against alpha-mannosidase (jack bean). These inhibitors were found to be more potent than the well-known inhibitors like kifunensine and deoxymannojirimycin based on docking and biochemi...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Sivapriya K,Hariharaputran S,Suhas VL,Chandra N,Chandrasekaran S

    更新日期:2007-09-01 00:00:00

  • A study on the conversion of indanones into carbostyrils.

    abstract::We have surveyed the utility of Beckmann rearrangement for the conversion of indanones into carbostyrils. Initial attempts at the conversion of 6-methoxy indanone oxime under classical conditions resulted in the formation of the two unusual products: 2-sulfonyloxyindanone and the dimeric product. This unusual rearrang...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Torisawa Y,Nishi T,Minamikawa Ji

    更新日期:2003-05-15 00:00:00

  • Three-dimensional quantitative structure-activity relationship (3D-QSAR) of 3-aryloxazolidin-2-one antibacterials.

    abstract::Three-dimensional quantitative structure-activity relationship (3D-QSAR) studies for 3-aryloxazolidin-2-one antibacterials were performed using the genetic function approximation algorithm. This study was performed using 60 compounds, in which the QSAR models were developed using a training set of 50 compounds. The in...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Karki RG,Kulkarni VM

    更新日期:2001-12-01 00:00:00

  • Synthesis and evaluation of macrocyclic amino acid derivatives for tumor imaging by gallium-68 positron emission tomography.

    abstract::(68)Ga PET imaging in clinical oncology represents a notable development because the availability of (68)Ga is not dependent on a cyclotron. Furthermore, labeled amino acid derivatives have been proven to be useful for the imaging many tumor types. In the present study, we synthesized β-aminoalanine, γ-aminohomoalanin...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Shetty D,Jeong JM,Ju CH,Kim YJ,Lee JY,Lee YS,Lee DS,Chung JK,Lee MC

    更新日期:2010-11-01 00:00:00

  • Antimalarial and antiproliferative evaluation of bis-steroidal tetraoxanes.

    abstract::Several cis and trans bis-steroidal 1,2,4,5-tetraoxanes possessing amide terminus were synthesised and evaluated as antimalarials and antiproliferatives. The compounds exhibited submicromolar antimalarial activity against Plasmodium falciparum D6 and W2 strains. The existence of HN-C(O) moiety was found necessary for ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Opsenica D,Angelovski G,Pocsfalvi G,Juranić Z,Zizak Z,Kyle D,Milhous WK,Solaja BA

    更新日期:2003-07-03 00:00:00

  • Discovery of platelet-type 12-human lipoxygenase selective inhibitors by high-throughput screening of structurally diverse libraries.

    abstract::Human lipoxygenases (hLO) have been implicated in a variety of diseases and cancers and each hLO isozyme appears to have distinct roles in cellular biology. This fact emphasizes the need for discovering selective hLO inhibitors for both understanding the role of specific lipoxygenases in the cell and developing pharma...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Deschamps JD,Gautschi JT,Whitman S,Johnson TA,Gassner NC,Crews P,Holman TR

    更新日期:2007-11-15 00:00:00

  • Synthesis and evaluation of oligo-1,3-thiazolecarboxamide derivatives as HIV-1 reverse transcriptase inhibitors.

    abstract::A set of oligo-1,3-thiazolecarboxamide derivatives able to interact with the minor groove of nucleic acids was synthesized. These oligopeptides contained different numbers of thiazole units presenting dimethylaminopropyl or EDTA moieties on the C-terminus, and aminohexanoyl or EDTA moieties on the N-terminus. The inhi...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Ryabinin VA,Zakharova OD,Yurchenko EY,Timofeeva OA,Martyanov IV,Tokarev AA,Belanov EF,Bormotov NI,Tarrago-Litvak L,Andreola ML,Litvak S,Nevinsky GA,Sinyakov AN

    更新日期:2000-05-01 00:00:00

  • Synthesis and evaluation of a series of 1,4-diarylbutadienes for anticoccidial activity.

    abstract::During the course of a collaborative screening program, a set of 1-phenyl-4-pyridyl-butadienes was found to exhibit in vitro activity against Eimeria tenella in a cell-based assay. Activity was dependent on the chain length and degree of unsaturation of the linker between the two aryl groups as well as substitution of...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Gage JL,Kirst HA,O'Neil D,David BA,Smith CK 2nd,Naylor SA

    更新日期:2003-09-01 00:00:00

  • N-phenethyl and N-naphthylmethyl isatins and analogues as in vitro cytotoxic agents.

    abstract::A range of N-phenethyl, N-phenacyl, and N-(1- and 2-naphthylmethyl) derivatives of 5,7-dibromoisatin 2 were prepared by N-alkylation reactions. Their activity against human monocyte-like histiocytic lymphoma (U937), leukemia (Jurkat), and breast carcinoma (MDA-MB-231) cell lines was assessed. The results allowed furth...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Matesic L,Locke JM,Bremner JB,Pyne SG,Skropeta D,Ranson M,Vine KL

    更新日期:2008-03-15 00:00:00

  • A convenient synthesis and hepatoprotective activity of imidazo[1,2-c]pyrimido[5,4-e]pyrimidine, tetraazaacenaphthene and tetraazaphenalene from cyclic ketene aminals through tandem addition-cyclization reactions.

    abstract::A novel one-pot synthesis of imidazo[1,2-c]pyrimido[5,4-e]pyrimidinones (2), tetraazaacenaphthene-3,6-diones (4), tetarazaphenalene-1,7-dione (4d) is delineated from the reaction of cyclic ketene aminal (1) and alkyl or aryl isothiocyanate through tandem addition-cyclization reactions. However, reaction of ketene amin...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Ram VJ,Goel A,Sarkhel S,Maulik PR

    更新日期:2002-05-01 00:00:00

  • Synthesis and structure based optimization of 2-(4-phenoxybenzoyl)-5-hydroxyindole as a novel CaMKII inhibitor.

    abstract::Based on 2-(4-phenoxybenzoyl)-5-hydroxyindole (2), a novel structural class of CaMKII inhibitors were synthesized and further optimized. The strong acidity of the hydroxyl group and the lipophilic group at the 4 and 6-positions were found to be necessary for strong CaMKII inhibition. Compound 25 was identified as a pr...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Komiya M,Asano S,Koike N,Koga E,Igarashi J,Nakatani S,Isobe Y

    更新日期:2012-12-01 00:00:00

  • Synthesis and cytotoxic activities of goniothalamins and derivatives.

    abstract::Substituted goniothalamins containing cyclopropane-groups were efficiently prepared in high yields and good selectivity. Antiproliferative activity was measured on three human cancer cell lines (A549, MCF-7, HBL-100), to show which of the structural elements of goniothalamins is mandatory for cytotoxicity. We found th...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Weber A,Döhl K,Sachs J,Nordschild ACM,Schröder D,Kulik A,Fischer T,Schmitt L,Teusch N,Pietruszka J

    更新日期:2017-11-15 00:00:00

  • Identification of novel benzimidazole derivatives as inhibitors of leukotriene biosynthesis by virtual screening targeting 5-lipoxygenase-activating protein (FLAP).

    abstract::Pharmacological suppression of leukotriene biosynthesis by 5-lipoxygenase (5-LO)-activating protein (FLAP) inhibitors is a promising strategy to intervene with inflammatory, allergic and cardiovascular diseases. Virtual screening targeting FLAP based on a combined ligand- and structure-based pharmacophore model led to...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Banoglu E,Çalişkan B,Luderer S,Eren G,Özkan Y,Altenhofen W,Weinigel C,Barz D,Gerstmeier J,Pergola C,Werz O

    更新日期:2012-06-15 00:00:00

  • Actin-binding doliculide causes premature senescence in p53 wild type cells.

    abstract::Addressing the actin cytoskeleton as future anticancer target can be an innovative chemotherapeutic approach to combat malignancies. Doliculide is a potent stabilizer of actin filaments and can be used as tool and therapeutic lead in cancer research. Though a variety of molecules are known to bind to actin and lead to...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Foerster F,Chen T,Altmann KH,Vollmar AM

    更新日期:2016-01-15 00:00:00

  • Hydroxy- or methoxy-substituted benzaldoximes and benzaldehyde-O-alkyloximes as tyrosinase inhibitors.

    abstract::Several benzaldoximes, benzaldehyde-O-ethyloximes, and acetophenonoximes were synthesized and evaluated as tyrosinase inhibitors by an assay based on tyrosinase catalyzed L-DOPA oxidation. Whereas benzaldoxime itself is only a weak inhibitor, its derivatives with one or two hydroxy or methoxy moieties in para and meta...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Ley JP,Bertram HJ

    更新日期:2001-07-01 00:00:00

  • Selective angiotensin II AT(2) receptor agonists devoid of the imidazole ring system.

    abstract::A versatile parallel synthetic method to obtain three series of non-cyclic analogues of the first drug-like selective angiotensin II AT(2) receptor agonist (1) has been developed. In analogy with the transformation of losartan to valsartan it was demonstrated that a non-cyclic moiety could be employed as an imidazole ...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Murugaiah AM,Wallinder C,Mahalingam AK,Wu X,Wan Y,Plouffe B,Botros M,Karlén A,Hallberg M,Gallo-Payet N,Alterman M

    更新日期:2007-11-15 00:00:00

  • Activation of anti-oxidant Nrf2 signaling by substituted trans stilbenes.

    abstract::Nrf2, which is a member of the cap'n'collar family of transcription factors, is a major regulator of phase II detoxification and anti-oxidant genes as well as anti-inflammatory and neuroprotective genes. The importance of inflammation and oxidative stress in many chronic diseases supports the concept that activation o...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Deck LM,Whalen LJ,Hunsaker LA,Royer RE,Vander Jagt DL

    更新日期:2017-02-15 00:00:00

  • A theoretical study on the structure-activity relationships of metabolites of folates as antioxidants and its implications for rational design of antioxidants.

    abstract::To elucidate the structure-activity relationships of metabolites of folates as antioxidants, the O-H bond dissociation enthalpies (BDEs) and ionization potentials (IPs) for these compounds were calculated by density functional theory (DFT) on B3LYP/6-31+G(,3pd) level. Accordingly, the antioxidant activity difference f...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Ji HF,Tang GY,Zhang HY

    更新日期:2005-02-15 00:00:00

  • Studies on anti-HIV quinolones: new insights on the C-6 position.

    abstract::The 6-desfluoroquinolones which have been developed by our group represent a promising class of compounds for the treatment of HIV infection since they act on transcriptional regulation, a crucial step in the replication cycle that has not been clinically exploited, yet. Focussing attention on the N-1 and C-6 position...

    journal_title:Bioorganic & medicinal chemistry

    pub_type: 杂志文章


    authors: Massari S,Daelemans D,Manfroni G,Sabatini S,Tabarrini O,Pannecouque C,Cecchetti V

    更新日期:2009-01-15 00:00:00