5-oxo-15-HETE: total synthesis and bioactivity.


:The first total synthesis of 6(E),8(Z),11(Z),13(E) 5-oxo-15-HETE 4 was accomplished. The synthetic material was evaluated with calcium mobilization assay and compared with 5-oxo-ETE the natural ligand for the OXE receptor.


Bioorg Med Chem Lett


Patel P,Anumolu JR,Powell WS,Rokach J




Has Abstract


2011-03-15 00:00:00














  • Polycyclic aromatic compounds as anticancer agents: synthesis and biological evaluation of some chrysene derivatives.

    abstract::Synthesis and biological evaluation of new chrysene derivatives aimed at the development of anticancer agents were carried out. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Becker FF,Banik BK

    更新日期:1998-10-20 00:00:00

  • The preparation of 2,6-disubstituted pyridinyl phosphine oxides as novel anti-cancer agents.

    abstract::A series of 2,6-dimethoxylpyridinyl phosphine oxides have been synthesized and examined for their antitumor activity. 2,6-Dimethoxy-3-phenyl-4-diphenylphosphinoylpyridine 2 has been employed as the lead compound for this study. We found out that the presence of phosphine oxide on the 2,6-dimethoxylpyridine ring is imp...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Lam KH,Gambari R,Yuen MC,Kan CW,Chan P,Xu L,Tang W,Chui CH,Cheng GY,Wong RS,Lau FY,Tong CS,Chan AK,Lai PB,Kok SH,Cheng CH,Chan AS,Tang JC

    更新日期:2009-04-15 00:00:00

  • Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazines.

    abstract::N-1-Alkylamino and N-1-alkyloxy-4-hydroxyquinolon-3-yl benzothiadiazines were synthesized and evaluated as inhibitors of genotype 1 HCV polymerase. The N-1-alkyloxy derivatives were not potent inhibitors, however N-1-alkylamino derivatives displayed comparable potency to carbon analogs. Analogs with aliphatic substitu...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Pratt JK,Donner P,McDaniel KF,Maring CJ,Kati WM,Mo H,Middleton T,Liu Y,Ng T,Xie Q,Zhang R,Montgomery D,Molla A,Kempf DJ,Kohlbrenner W

    更新日期:2005-03-15 00:00:00

  • Synthesis of Vorinostat and cholesterol conjugate to enhance the cancer cell uptake selectivity.

    abstract::Histone deacetylase (HDAC) inhibitors modulate various cellular functions including proliferation, differentiation, and apoptosis. Vorinostat (SuberAniloHydroxamic Acid, SAHA) is the first HDAC inhibitor approved by FDA for cancer treatment. However, SAHA distributes in cancer tissue and normal tissue in similar level...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Idippily ND,Gan C,Orefice P,Peterson J,Su B

    更新日期:2017-02-15 00:00:00

  • Synthesis and antimalarial activity of calothrixins A and B, and their N-alkyl derivatives.

    abstract::We synthesized calothrixin B using our developed biomimetic method and derived N-alkyl-calothrixins A and B. The in vitro antimalarial activity of the calothrixin derivatives, including calothrixins A and B, against the Plasmodium falciparum FCR-3 strain was evaluated. All test compounds exhibited antimalarial activit...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Matsumoto K,Choshi T,Hourai M,Zamami Y,Sasaki K,Abe T,Ishikura M,Hatae N,Iwamura T,Tohyama S,Nobuhiro J,Hibino S

    更新日期:2012-07-15 00:00:00

  • Benzimidazole-carboxamides as potent and bioavailable stearoyl-CoA desaturase (SCD1) inhibitors from ligand-based virtual screening and chemical optimization.

    abstract::The discovery of potent benzimidazole stearoyl-CoA desaturase (SCD1) inhibitors by ligand-based virtual screening is described. ROCS 3D-searching gave a favorable chemical motif that was subsequently optimized to arrive at a chemical series of potent and promising SCD1 inhibitors. In particular, compound SAR224 was se...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Matter H,Zoller G,Herling AW,Sanchez-Arias JA,Philippo C,Namane C,Kohlmann M,Pfenninger A,Voss MD

    更新日期:2013-03-15 00:00:00

  • Pyridoxine as a template for the design of antiplatelet agents.

    abstract::The B(6) vitamers have been shown to display beneficial therapeutic effects in cardiovascular related disorders. The design of novel antiplatelet agents using pyridoxine as a template has led to the discovery of a class of novel cardio- and cerebro-protective agents. The present study describes the synthesis of severa...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Zhang W,Yao J,Pham V,Whitney T,Froese D,Friesen A,Stang L,Xu C,Shuaib A,Diakur JM,Haque W

    更新日期:2004-09-20 00:00:00

  • Design of novel lipidated peptidomimetic conjugates for targeting EGFR heterodimerization in HER2 + cancer.

    abstract::The human epidermal growth factor receptor (EGFR) family is known to be involved in cell signaling pathways. The extracellular domain of EGFR consists of four domains, of which domain II and domain IV are known to be involved in the dimerization process. Overexpression of these receptors is known to play a significant...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Naik H,Gauthier T,Singh S,Jois S

    更新日期:2018-12-01 00:00:00

  • Synthesis of H-bonding probes of alpha7 nAChR agonist selectivity.

    abstract::The alpha7 subtype of the nicotinic acetylcholine receptor (nAChR) is the target of studies aimed at identifying features that will lead to the development of selective therapeutics. Five arylidine anabaseines, three with pyridine rings and two with the pyrrole rings, were synthesized in 35-65% yield via aldol condens...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Wang J,Papke RL,Horenstein NA

    更新日期:2009-01-15 00:00:00

  • Substituted aminobenzimidazole pyrimidines as cyclin-dependent kinase inhibitors.

    abstract::A series of aminobenzimidazole-substituted pyrimidines were synthesized and evaluated for biochemical activity against CDK1. A high-speed parallel synthesis approach enabled the identification of a potent lead series having improved potency in the CDK1 assay (IC(50)<10nM). Cell cycle analysis showed that the compounds...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Verma S,Nagarathnam D,Shao J,Zhang L,Zhao J,Wang Y,Li T,Mull E,Enyedy I,Wang C,Zhu Q,Altieri M,Jordan J,Dang TT,Reddy S

    更新日期:2005-04-15 00:00:00

  • pH-Dependant fluorescence switching of an i-motif structure incorporating an isomeric azobenzene/pyrene fluorophore.

    abstract::In this study, we synthesized an Azo-py phosphoramidite, featuring azobenzene and pyrene units, as a novel fluorescent and isomeric (trans- and cis-azobenzene units) material, which we incorporated in an i-motif DNA sequence. We then monitored the structural dynamics and changes in fluorescence as the modified DNA seq...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Joo HN,Van Thi Nguyen T,Chae HK,Seo YJ

    更新日期:2017-06-01 00:00:00

  • Synthesis of thiophene-2-carboxamidines containing 2-aminothiazoles and their biological evaluation as urokinase inhibitors.

    abstract::The serine protease urokinase (uPa) has been implicated in the progression of both breast and prostate cancer. Utilizing structure based design, the synthesis of a series of substituted 4-[2-amino-1,3-thiazolyl]-thiophene-2-carboxamidines is described. Further optimization of this series by substitution of the termina...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Wilson KJ,Illig CR,Subasinghe N,Hoffman JB,Rudolph MJ,Soll R,Molloy CJ,Bone R,Green D,Randall T,Zhang M,Lewandowski FA,Zhou Z,Sharp C,Maguire D,Grasberger B,DesJarlais RL,Spurlino J

    更新日期:2001-04-09 00:00:00

  • Synthesis of potent taxoids for tumor-specific delivery using monoclonal antibodies.

    abstract::The targeted delivery of taxoids, in the form of taxane-antibody immunoconjugates, requires the preparation of taxoids containing moieties suitable for their conjugation to monoclonal antibodies. A series of taxoids incorporating a disulfide-containing linker at various positions of the taxoid framework have been prep...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Miller ML,Roller EE,Wu X,Leece BA,Goldmacher VS,Chari RV,Ojima I

    更新日期:2004-08-02 00:00:00

  • Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.

    abstract::Coexpression of EGFR and HER2 has been found in many tumors such as breast, ovarian, colon and prostate cancers, with poor prognosis of the patients. Herein, our team has designed and synthesized new eighteen compounds with 6-substituted 4-anilinoquinazoline core to selectively inhibit EGFR/HER2 tyrosine kinases. Twel...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Elkamhawy A,Farag AK,Viswanath AN,Bedair TM,Leem DG,Lee KT,Pae AN,Roh EJ

    更新日期:2015-11-15 00:00:00

  • Identification of a novel series of selective 5-HT7 receptor antagonists.

    abstract::Novel 5-HT(7) receptor antagonists containing the benzocycloheptanone core were identified from high throughput screening. Molecular modelling and SAR studies have converted these intractable hits into a more potent, selective and tractable series, exemplified by compound (25), SB-691673. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Forbes IT,Cooper DG,Dodds EK,Douglas SE,Gribble AD,Ife RJ,Lightfoot AP,Meeson M,Campbell LP,Coleman T,Riley GJ,Thomas DR

    更新日期:2003-03-24 00:00:00

  • Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists.

    abstract::Novel (E)-N(1)-(benzyl)cinnamamidines were prepared and evaluated as NR2B subtype NMDA receptor ligands. Excellent affinity was achieved by appropriate substitution of either phenyl ring. The 2-methoxybenzyl compound 1h had approximately 1,000-fold lower IC(50) in NR2B than NR2A-containing cells. Replacement of the st...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Curtis NR,Diggle HJ,Kulagowski JJ,London C,Grimwood S,Hutson PH,Murray F,Richards P,Macaulay A,Wafford KA

    更新日期:2003-02-24 00:00:00

  • Synthesis, in vitro inhibitory activity towards COX-2 and haemolytic activity of derivatives of esculentoside A.

    abstract::Esculentoside A (EsA) has been reported to possess anti-inflammatory activity and selective inhibitory activity towards cyclooxygenase-2. A series of derivatives of EsA were synthesized by converting the C-28 carboxylic acid group into amides. The haemolytic activity and inhibitory activity towards cyclooxygenase-2 we...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Wu F,Yi Y,Sun P,Zhang D

    更新日期:2007-12-01 00:00:00

  • Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.

    abstract::New N-(1,2-diphenylethyl)piperazines 6 are disclosed as dual serotonin and noradrenaline reuptake inhibitors (SNRI) which may have potential in treating stress urinary incontinence (SUI). In this Letter, we present new data for SNRI PF-526014 (4) including performance in a canine in vivo model of SUI, cardiovascular a...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Fray MJ,Fish PV,Allan GA,Bish G,Clarke N,Eccles R,Harrison AC,Le Net JL,Phillips SC,Regan N,Sobry C,Stobie A,Wakenhut F,Westbrook D,Westbrook SL,Whitlock GA

    更新日期:2010-06-15 00:00:00

  • Selective heterocyclic amidine inhibitors of human inducible nitric oxide synthase.

    abstract::The potency and selectivity of a series of 5-hetero-2-iminohexahydroazepines were examined as inhibitors of the three human NOS isoforms. The effect of ring substitution of the 5-carbon for a heteroatom is presented. Potencies (IC(50)'s) for these inhibitors are in the low micromolar range for hi-NOS with some example...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Moormann AE,Metz S,Toth MV,Moore WM,Jerome G,Kornmeier C,Manning P,Hansen DW Jr,Pitzele BS,Webber RK

    更新日期:2001-10-08 00:00:00

  • Synthesis, iron binding and antimicrobial properties of hexadentate 3-hydroxypyridinones-terminated dendrimers.

    abstract::Macromolecular chelators have potential applications in the medical area, for instance, in treatment of iron overload-related disorders and in the treatment of external infections. In this investigation, several novel iron(III)-selective hydroxypyridinone hexadentate-terminated first and second generation dendrimeric ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Zhou T,Chen K,Kong LM,Liu MS,Ma YM,Xie YY,Hider RC

    更新日期:2018-08-01 00:00:00

  • Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.

    abstract::New RXR-selective modulators possessing a 6-fluoro trienoic acid moiety (6Z olefin) or a fluorinated/heterocyclic-substituted benzene core ring, were synthesized in an expedient and selective way. A subset of these compounds was evaluated for their metabolic properties (exposure in IRC male mice) and show a dramatic i...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Michellys PY,Boehm MF,Chen JH,Grese TA,Karanewsky DS,Leibowitz MD,Liu S,Mais DA,Mapes CM,Reifel-Miller A,Ogilvie KM,Rungta D,Thompson AW,Tyhonas JS,Yumibe N,Ardecky RJ

    更新日期:2003-11-17 00:00:00

  • Synthesis of rare sugars with L-fuculose-1-phosphate aldolase (FucA) from Thermus thermophilus HB8.

    abstract::We report herein a one-pot four-enzyme approach for the synthesis of the rare sugars d-psicose, d-sorbose, l-tagatose, and l-fructose with aldolase FucA from a thermophilic source (Thermus thermophilus HB8). Importantly, the cheap starting material DL-GP (DL-glycerol 3-phosphate), was used to significantly reduce the ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Li Z,Cai L,Qi Q,Styslinger TJ,Zhao G,Wang PG

    更新日期:2011-09-01 00:00:00

  • Synthesis and biological evaluation of benzazepine oxazolidinone antibacterials.

    abstract::Novel benzazepine oxazolidinone antibacterials were synthesized and evaluated against clinically relevant susceptible and resistant organisms. The effect of ring nitrogen position and N-substitution on antibacterial activity is examined. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Johnson PD,Aristoff PA,Zurenko GE,Schaadt RD,Yagi BH,Ford CW,Hamel JC,Stapert D,Moerman JK

    更新日期:2003-12-01 00:00:00

  • Discovery of furan carboxylate derivatives as novel inhibitors of ATP-citrate lyase via virtual high-throughput screening.

    abstract::The enzyme ATP citrate lyase (ACL) catalyzes the formation of cytosolic acetyl CoA, the starting material for de novo lipid and cholesterol biosynthesis. The dysfunction and upregulation of ACL in numerous cancers makes it an attractive target for developing anticancer therapies. ACL inhibition by shRNA knockdown limi...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Jernigan FE,Hanai JI,Sukhatme VP,Sun L

    更新日期:2017-02-15 00:00:00

  • Synthesis and biological evaluation of deoxy-hematoxylin derivatives as a novel class of anti-HIV-1 agents.

    abstract::SAR studies for the exploration a novel class of anti-human immunodeficiency virus type 1 (HIV-1) agents based on the hematoxylin structure (1) are described. The systematic deoxygenations of 1 including asymmetric synthesis were conducted to obtain a compound showing high potencies for inhibiting the nuclear import a...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Ishii H,Koyama H,Hagiwara K,Miura T,Xue G,Hashimoto Y,Kitahara G,Aida Y,Suzuki M

    更新日期:2012-02-01 00:00:00

  • Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.

    abstract::The synthesis and SAR of a series of novel pyrazolo-quinazolines as potent and selective MPS1 inhibitors are reported. We describe the optimization of the initial hit, identified by screening the internal library collection, into an orally available, potent and selective MPS1 inhibitor. ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Caldarelli M,Angiolini M,Disingrini T,Donati D,Guanci M,Nuvoloni S,Posteri H,Quartieri F,Silvagni M,Colombo R

    更新日期:2011-08-01 00:00:00

  • Synthesis and evaluation of cholecystokinin trimers: a multivalent approach to pancreatic cancer detection and treatment.

    abstract::In the quest for novel tools for early detection and treatment of cancer, we propose the use of multimers targeting overexpressed receptors at the cancer cell surface. Indeed, multimers are prone to create multivalent interactions, more potent and specific than their corresponding monovalent versions, thus enabling th...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Brabez N,Nguyen KL,Saunders K,Lacy R,Xu L,Gillies RJ,Lynch RM,Chassaing G,Lavielle S,Hruby VJ

    更新日期:2013-04-15 00:00:00

  • Discovery of 4-aminomethylphenylacetic acids as γ-secretase modulators via a scaffold design approach.

    abstract::Starting from literature examples of nonsteroidal anti-inflammatory drugs (NSAIDs)-type carboxylic acid γ-secretase modulators (GSMs) and using a scaffold design approach, we identified 4-aminomethylphenylacetic acid 4 with a desirable γ-secretase modulation profile. Scaffold optimization led to the discovery of a nov...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Xin Z,Peng H,Zhang A,Talreja T,Kumaravel G,Xu L,Rohde E,Jung MY,Shackett MN,Kocisko D,Chollate S,Dunah AW,Snodgrass-Belt PA,Arnold HM,Taveras AG,Rhodes KJ,Scannevin RH

    更新日期:2011-12-15 00:00:00

  • Benzyloxybenzaldehyde analogues as novel adenylyl cyclase activators.

    abstract::Several benzyloxybenzaldehyde analogues were prepared and found to have significant inhibitory activity toward neutrophil superoxide formation. Consequently, these compounds were evaluated for cAMP-elevating capability. Among them, benzyloxybenzaldehyde (7), exhibiting activity equivalent to forskolin, was determined ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Chang C,Kuo S,Lin Y,Wang J,Huang L

    更新日期:2001-08-06 00:00:00

  • Studies on the structure-activity relationship of 2',6'-dimethyl-l-tyrosine (Dmt) derivatives: bioactivity profile of H-Dmt-NH-CH(3).

    abstract::The 2',6'-dimethyl-l-tyrosine (Dmt) enhances receptor affinity, functional bioactivity and in vivo analgesia of opioid peptides. To further investigate its direct influence on these opioid parameters, we developed a series of compounds (H-Dmt-NH-X). Among them, H-Dmt-NH-CH(3) showed the highest affinity (K(i)mu=7.45 n...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Fujita Y,Tsuda Y,Motoyama T,Li T,Miyazaki A,Yokoi T,Sasaki Y,Ambo A,Niizuma H,Jinsmaa Y,Bryant SD,Lazarus LH,Okada Y

    更新日期:2005-02-01 00:00:00