Synthesis of (Z)-2-((1H-indazol-3-yl)methylene)-6-[¹¹C]methoxy-7-(piperazin-1-ylmethyl)benzofuran-3(2H)-one as a new potential PET probe for imaging of the enzyme PIM1.

abstract：:Starting with a micromolar lead identified from high-throughput screening, a series of pyrazoles were discovered with significantly improved potency on bacterial methionyl-tRNA synthetase and selectivity over human methionyl-tRNA synthetase. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Finn J,Mattia K,Morytko M,Ram S,Yang Y,Wu X,Mak E,Gallant P,Keith D

更新日期：2003-07-07 00:00:00

abstract：:A new method for the synthesis of 2'-O-methyl-2-thiouridine (s2Um) found in thermophilic bacterial tRNA was developed. Structural properties of s2Um and s2Um(p)U were studied by using 1H NMR spectroscopy. A modified nonaribonucleotide (RNA*: 5'-CGUUs2UmUUGC-3') was synthesized to study the base-recognition ability of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shohda K,Okamoto I,Wada T,Seio K,Sekine M

更新日期：2000-08-21 00:00:00

abstract：:Cancer cells isolated from two patients with malignant non-Hodgkin B-cell lymphomas that became resistant to chemotherapy during clinical treatment were made ≥fourfold resistant in culture to anticancer drugs, that is cisplatin, etoposide, methotrexate and bortezomib. Because most resistant lines showed significantly ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Schulz R,Emmrich T,Lemmerhirt H,Leffler U,Sydow K,Hirt C,Kiefer T,Link A,Bednarski PJ

更新日期：2012-11-01 00:00:00

abstract：:Elevated triglycerides (TG) contribute towards increased risk for cardiovascular disease. Lipoprotein lipase (LPL) is an enzyme that is responsible for the metabolism of core triglycerides of very-low density lipoproteins (VLDL) and chylomicrons in the vasculature. In this study, we explored the structure-activity rel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Geldenhuys WJ,Caporoso J,Leeper TC,Lee YK,Lin L,Darvesh AS,Sadana P

更新日期：2017-01-15 00:00:00

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

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

abstract：:Certain gamma-aryloxymethyl-alpha-methylene-gamma-phenyl- gamma-butyrolactones were synthesized and evaluated for their anticancer activity. These compounds demonstrated a strong growth inhibitory activity against leukemia cell lines but are relatively inactive against non-small cell lung cancers and CNS cancers. The ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang TC,Lee KH,Chen YL,Liou SS,Tzeng CC

更新日期：1998-10-06 00:00:00

abstract：:The first demonstration of DNA cleavage by resveratrol '3,5,4'-trihydroxy-trans-stilbene' is presented. Resveratrol mediated relaxation of pBR322 at micromolar concentrations in the presence of Cu2+. Evidence is provided that resveratrol is capable of binding to DNA, and that the Cu(2+)-dependent DNA damage is more li...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fukuhara K,Miyata N

更新日期：1998-11-17 00:00:00

abstract：:A series of a novel hybrid compounds between nitazoxanide and N-methylbenzimidazole were synthesized starting from the corresponding N-methyl-2-nitroanilines. The new hybrid compounds (1-13) were evaluated in vitro against Giardia intestinalis, Entamoeba histolytica, Trichomonas vaginalis. NTZ, MTZ and ABZ were used a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Soria-Arteche O,Hernández-Campos A,Yépez-Mulia L,Trejo-Soto PJ,Hernández-Luis F,Gres-Molina J,Maldonado LA,Castillo R

更新日期：2013-12-15 00:00:00

abstract：:In an effort to expand the spectrum of antibacterial activity associated with piperidin-4-one derivatives, we have synthesized two series of 3-carboxyethyl-2,6-diphenyl-4-hydroxy-Delta(3)-tetrahydropyridine derivatives bearing diversified heterocyclic and aromatic systems at the nitrogen atom through acetyl (6-18) and...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aridoss G,Amirthaganesan S,Jeong YT

更新日期：2010-04-01 00:00:00

abstract：:The use of the triterpenoid lupeol as a scaffold for the synthesis of lupeol-based libraries is described. Lupeol was anchored to a solid support (Rink amide/Sieber Amide) through aliphatic dicarboxylic acid moieties, which also served as a site for introducing diversity. The resulting polymer linked 3beta-O (resin-al...

journal_title：Bioorganic & medicinal chemistry letters

authors： Srinivasan T,Srivastava GK,Pathak A,Batra S,Raj K,Singh K,Puri SK,Kundu B

更新日期：2002-10-21 00:00:00

abstract：:The synthesis of steroid hormones is critical to human physiology and improper regulation of either the synthesis of these key molecules or activation of the associated receptors can lead to disease states. This has led to intense interest in developing compounds capable of modulating the synthesis of steroid hormones...

journal_title：Bioorganic & medicinal chemistry letters

authors： Blass BE,Iyer P,Abou-Gharbia M,Childers WE,Gordon JC,Ramanjulu M,Morton G,Arumugam P,Boruwa J,Ellingboe J,Mitra S,Reddy Nimmareddy R,Paliwal S,Rajasekhar J,Shivakumar S,Srivastava P,Tangirala RS,Venkataramanaiah K,Bob

更新日期：2018-07-15 00:00:00

abstract：:A novel glycosphingolipid, beta-D-GalNAcp(1-->4)[alpha-D- Fucp(1-->3)]-beta-D-GlcNAcp(1-->)Cer (1), isolated from the marine sponge Aplysinella rhax, has a unique structure, with D-fucose and N-acetyl-D-galactosamine attached to a reducing-end N-acetyl-D-glucosamine through an alpha1-->3 and beta1-->4 linkage, respect...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hada N,Nakashima T,Shrestha SP,Masui R,Narukawa Y,Tani K,Takeda T

更新日期：2007-11-01 00:00:00

abstract：:Synthesis of nitrone derivatives of trolox is described. Their biological evaluation was performed in vitro for scavenging different free radicals, inhibiting Fe(2+)-induced lipid peroxidation, and in vivo in a permanent middle cerebral artery occlusion model in mice. New compounds exert pharmacological activities com...

journal_title：Bioorganic & medicinal chemistry letters

authors： Balogh GT,Vukics K,Könczöl A,Kis-Varga A,Gere A,Fischer J

更新日期：2005-06-15 00:00:00

abstract：:The in vitro evaluation of a series of saturated prostaglandins revealed that compounds with omega chain aromatic rings retain nanomolar potency for the human prostaglandin F receptor (hFP receptor), exemplified by compound 8. In contrast, the double bonds are required for activity in the series with an acyclic omega ...

journal_title：Bioorganic & medicinal chemistry letters

authors： deLong MA,Amburgey J,Taylor C,Wos JA,Soper DL,Wang Y,Hicks R

更新日期：2000-07-17 00:00:00

abstract：:As part of a programme to identify further analogues of the dual topo I/II inhibitor XR11576, we describe here the syntheses and SAR studies of various 'minimal' and 3,4-benzofused phenazine chromophores of the phenazine template of XR11576. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang S,Miller W,Milton J,Vicker N,Stewart A,Charlton P,Mistry P,Hardick D,Denny WA

更新日期：2002-02-11 00:00:00

abstract：:Two novel chemical classes of kappa opioid receptor agonists, chroman-2-carboxamide derivatives and 2,3-dihydrobenzofuran-2-carboxamide derivatives, were synthesized. These agents exhibited high and selective affinity for the kappa opioid receptor. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chu GH,Gu M,Cassel JA,Belanger S,Graczyk TM,DeHaven RN,Conway-James N,Koblish M,Little PJ,DeHaven-Hudkins DL,Dolle RE

更新日期：2005-12-01 00:00:00

abstract：:A newly designed curcumin mimic library (11a-11k) with 2-ethylamino groups in a chalcone structure and variously substituted triazole groups as side chains was synthesized using the Huisgen 1,3-cycloaddition reaction between various alkynes (a-k) and an intermediate (10), with CuSO4 and sodium ascorbate in a solution ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ahn Y,Oh S,Lee SJ,Park BG,Park YS,Shin WS,Jang HJ,Park JH,Kwon D,Lee S

更新日期：2014-08-01 00:00:00

abstract：:Forty caffeate analogues were synthesized via a convenient method starting from vanillin with moderate to good yields. The testing of biological activity of these compounds against HIV-1 integrase indicates that four compounds: bornyl caffeate, bornyl 2-nitrocaffeate, 5-nitrocaffeic acid and 5-nitrocaffeic acid phenet...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xia CN,Li HB,Liu F,Hu WX

更新日期：2008-12-15 00:00:00

abstract：:A series of transdermal permeation enhancers based on dicarboxylic acid esters was studied. Single-chain amphiphiles were markedly more effective than the double-chain ones. Monododecyl maleate, that is a cis derivative, was a more potent enhancer than its trans isomer, while the activity of succinates strongly depend...

journal_title：Bioorganic & medicinal chemistry letters

authors： Novotný M,Hrabálek A,Janůsová B,Novotný J,Vávrová K

更新日期：2009-01-15 00:00:00

abstract：:Chemical investigation of a marine-derived fungus Penicillium sp. SF-6013 resulted in the discovery of a new tanzawaic acid derivative, 2E,4Z-tanzawaic acid D (1), together with four known analogues, tanzawaic acids A (2) and D (3), a salt form of tanzawaic acid E (4), and tanzawaic acid B (5). Their structures were m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Quang TH,Ngan NTT,Ko W,Kim DC,Yoon CS,Sohn JH,Yim JH,Kim YC,Oh H

更新日期：2014-12-15 00:00:00

abstract：:A series of optically pure phenyl-and non-phenyl-substituted 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(2-hydroxypropyl)piperazines was synthesized and their binding affinity for dopamine transporter (DAT) was investigated. The analogues with a hydroxyl group in the S configuration were more selective for the DAT over...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hsin LW,Prisinzano T,Wilkerson CR,Dersch CM,Horel R,Jacobson AE,Rothman RB,Rice KC

更新日期：2003-02-10 00:00:00

abstract：:The structure-based design and synthesis of isothiazolidinone (IZD) inhibitors of PTP1B containing imidazoles and imidazolines and their modification to interact with the B site of PTP1B are described here. The X-ray crystal structures of 3I and 4I complexed with PTP1B were solved and revealed the inhibitors are inter...

journal_title：Bioorganic & medicinal chemistry letters

authors： Douty B,Wayland B,Ala PJ,Bower MJ,Pruitt J,Bostrom L,Wei M,Klabe R,Gonneville L,Wynn R,Burn TC,Liu PC,Combs AP,Yue EW

更新日期：2008-01-01 00:00:00

abstract：:Mass-directed isolation of the CH(2)Cl(2)/MeOH extract from the leaves of Cryptocarya obovata resulted in the purification of a new trypanocidal alpha-pyrone, 7',8'-dihydroobolactone (1). The chemical structure of 1 was determined by 1D/2D NMR, MS and CD data analysis. 7',8'-Dihydroobolactone was shown to inhibit Tryp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Davis RA,Demirkiran O,Sykes ML,Avery VM,Suraweera L,Fechner GA,Quinn RJ

更新日期：2010-07-15 00:00:00

abstract：:Resistance of malaria parasites has quickly developed to almost all used antimalarial drugs. Accordingly, the discovery of new effective drugs to counter the spread of malaria parasites that are resistant to existing agents, especially acting on multi-targets, is an urgent need. The cysteine protease falcipain-2 (FP-2...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang H,Lu W,Li X,Cong X,Ma H,Liu X,Zhang Y,Che P,Ma R,Li H,Shen X,Jiang H,Huang J,Zhu J

更新日期：2012-01-15 00:00:00

abstract：:Synthesis of the potent antiplasmodial 4-aminoquinoline, phenylequine (PQ), is reported for the first time. PQ and the two analogues show increased efficacy in moving from the chloroquine sensitive D10 to the chloroquine resistant K1 strain in vitro. The in vivo efficacy of PQ, and salts thereof, have been determined ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Blackie MA,Yardley V,Chibale K

更新日期：2010-02-01 00:00:00

abstract：:Bioassay-guided fractionation of the fruit powder of graviola (Annona muricata) yielded three novel compounds: muricins J, K, and L. The compounds are all C35 Annonaceous acetogenins with a mono-tetrahydrofuran ring and four hydroxyls. Their structures were elucidated by spectral methods and chemical modification afte...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sun S,Liu J,Kadouh H,Sun X,Zhou K

更新日期：2014-06-15 00:00:00

abstract：:The blood-brain barrier choline transporter may have utility as a drug delivery vector to the central nervous system. Surprisingly, this transporter has as yet not been cloned and expressed. We therefore initiated a 3D-QSAR study to develop predictive models for compound binding and identify structural features import...

journal_title：Bioorganic & medicinal chemistry letters

authors： Geldenhuys WJ,Lockman PR,McAfee JH,Fitzpatrick KT,Van der Schyf CJ,Allen DD

更新日期：2004-06-21 00:00:00

abstract：:By recruiting the important moiety from Shikonin, a series of novel oxoindoline derivatives S1-S20 have been synthesized for inhibiting H. pylori urease. The most potent compound S18 displayed better activity (IC50 = 0.71 μM; MIC = 0.48 μM) than the positive controls AHA (IC50 = 17.2 μM) and Metronidazole (MIC = 31.3 ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang YS,Su MM,Zhang XP,Liu QX,He ZX,Xu C,Zhu HL

更新日期：2018-10-15 00:00:00

abstract：:The stereoselective synthesis and biological activity of NPS 1407 (4a), (S)-(-)-3-amino-1,1-bis(3-fluorophenyl)butane, a potent, stereoselective antagonist of the NMDA receptor, are described. The racemate (4) was found to be active at the NMDA receptor in an in vitro assay, prompting the synthesis of the individual s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Moe ST,Smith DL,DelMar EG,Shimizu SM,Van Wagenen BC,Balandrin MF,Chien YE,Raszkiewicz JL,Artman LD,White HS,Mueller AL

更新日期：2000-11-06 00:00:00

abstract：:Ceramides are the major lipid components of the stratum corneum, the major permeability barrier of the skin. Here we report a chemical synthesis of ceramide analogs covalently bonded on the silica particles, that can be used to predict the skin permeability of chemicals via HPLC methods. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yin J,Liu H,Pidgeon C

更新日期：1998-01-20 00:00:00