InCl3 mediated one-pot multicomponent synthesis, anti-microbial, antioxidant and anticancer evaluation of 3-pyranyl indole derivatives.

abstract：:In this study we report the synthesis and activity against bovine viral diarrhea virus (BVDV) of a novel series of bicycle δ-sultones containing γ-lactones. BVDV is responsible for major losses in cattle. Some of the synthesized δ-sultones showed pronounced anti-BVDV activity with EC50 values of 0.12-1.0μM and no sign...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu HW,Zhao LJ,Liu HF,Zhao D,Luo J,Xie XP,Liu WS,Zheng JX,Dai GF,Liu HM,Liu LH,Liang YB

更新日期：2014-05-15 00:00:00

abstract：:This Letter describes, for the first time, the synthesis and SAR, developed through an iterative analog library approach, that led to the discovery of the positive allosteric modulator (PAM) of the metabotropic glutamate receptor mGluR5 CPPHA. Binding to a unique allosteric binding site distinct from other mGluR5 PAMs...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhao Z,Wisnoski DD,O'Brien JA,Lemaire W,Williams DL Jr,Jacobson MA,Wittman M,Ha SN,Schaffhauser H,Sur C,Pettibone DJ,Duggan ME,Conn PJ,Hartman GD,Lindsley CW

更新日期：2007-03-01 00:00:00

abstract：:Nrf2 is the major transcription factor that regulates many of the cytoprotective enzymes involved in the adaptive stress response. Modulation of Nrf2 could be therapeutically useful in a number of disease states. Activation can occur through either an electrophilic or non-electrophilic mechanism. To date, most of the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Richardson BG,Jain AD,Speltz TE,Moore TW

更新日期：2015-06-01 00:00:00

abstract：:A series of sesquiterpene compounds possessing both eudesmane and eremophilane skeletons were tested as gastric cytoprotective agents on male Wistar rats. The presence of an alpha,beta-unsaturated aldehyde on the C-7 side chain together with a hydroxyl group at C-4 is the requirement for the observed antiulcerogenic a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Donadel OJ,Guerreiro E,María AO,Wendel G,Enriz RD,Giordano OS,Tonn CE

更新日期：2005-08-01 00:00:00

abstract：:High potency pyrazole-based noncovalent inhibitors of human cathepsin S (CatS) were developed by modification of the benzo-fused 5-membered ring heterocycles found in earlier series of CatS inhibitors. Although substitutions on this heterocyclic framework had a moderate impact on enzymatic potency, dramatic effects on...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wei J,Pio BA,Cai H,Meduna SP,Sun S,Gu Y,Jiang W,Thurmond RL,Karlsson L,Edwards JP

更新日期：2007-10-15 00:00:00

abstract：:A series of potent non-acetylinic negative allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5 NAMs) was developed starting from HTS screening hit 1. Potency was improved via iterative SAR, and physicochemical properties were optimized to deliver orally bioavailable compounds acceptable for in vivo t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Duvey G,Perry B,Le Poul E,Poli S,Bonnet B,Lambeng N,Charvin D,Donovan-Rodrigues T,Haddouk H,Gagliardi S,Rocher JP

更新日期：2013-08-15 00:00:00

abstract：:A new solid-phase synthesis for ET receptor antagonists suitable for automation is presented. A support bound 2-hydroxybutyric acid derivative was converted to the corresponding ether derivatives using 4-halo-2-methylsulfonylpyrimidines. Subsequent Suzuki coupling with various aryl boronic acids gave the desired antag...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lange UE,Braje WM,Amberg W,Kettschau G

更新日期：2003-05-19 00:00:00

abstract：:Cage amines 1-4 are potent peripheral anionic site-bound reversible inhibitors of both acetylcholinesterase and butyrylcholinesterase. Cage amines 1-3 are selective butyrylcholinesterase inhibitor versus acetylcholinesterase. For both enzymes, the -log K(i) values linearly correlate with the difference of substituted ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lin G,Tsai HJ,Tsai YH

更新日期：2003-09-01 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：:It is well known that resveratrol (RSV) displayed cancer-preventing and anticancer properties but its clinical application is limited because of a low bioavailability and a rapid clearance from the circulation. Aim of this work was to synthesize pharmacologically active resveratrol analogs with an enhanced structural ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sala M,Chimento A,Saturnino C,Gomez-Monterrey IM,Musella S,Bertamino A,Milite C,Sinicropi MS,Caruso A,Sirianni R,Tortorella P,Novellino E,Campiglia P,Pezzi V

更新日期：2013-09-01 00:00:00

abstract：:Ligand efficient fragments binding to PDK1 were identified by an NMR fragment-based screening approach. Computational modeling of the fragments bound to the active site led to the design and synthesis of a series of novel 6,7-disubstituted thienopyrimidin-4-one compounds, with low micromolar inhibitory activity agains...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee AC,Ramanujulu PM,Poulsen A,Williams M,Blanchard S,Ma DM,Bonday Z,Goh KL,Goh KC,Goh MK,Wood J,Dymock BW

更新日期：2012-06-15 00:00:00

abstract：:The syntheses and SAR investigations of novel CB(1) receptor antagonists based on a 1,2-diaryl piperidine core have been described. Optimization of this core afforded a compound with robust in vivo potency by reducing food intake in a mouse DIO model. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Scott JD,Li SW,Wang H,Xia Y,Jayne CL,Miller MW,Duffy RA,Boykow GC,Kowalski TJ,Spar BD,Stamford AW,Chackalamannil S,Lachowicz JE,Greenlee WJ

更新日期：2010-02-01 00:00:00

abstract：:Novel prostaglandin E2 receptor 4 (EP4) agonists featuring a pyridone core and an allylic alcohol ω-chain were discovered. These agonists were shown to be selective over EP1, EP2 and EP3. Analogs harboring a 4-carboxylic acid phenethyl α-chain displayed improved potency over those containing an n-heptanoic acid chain....

journal_title：Bioorganic & medicinal chemistry letters

authors： Dorich S,Cox JH,Burch JD,Chagnon F,Chen B,Léger S,St-Onge M,Fader LD

更新日期：2020-05-15 00:00:00

abstract：:Inhibition of 11beta-HSD1 has demonstrated potential in the treatment of various components of metabolic syndrome. We wish to report herein the discovery of novel azabicyclic sulfonamide based 11beta-HSD1 inhibitors. Highly potent compounds exhibiting inhibitory activities at both human and mouse 11beta-HSD1 were iden...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shah U,Boyle CD,Chackalamannil S,Baker H,Kowalski T,Lee J,Terracina G,Zhang L

更新日期：2010-03-01 00:00:00

abstract：:The synthesis of three series of quinol fatty alcohols (QFAs) and their biological activities on the promotion of axonal growth are described. Interestingly, the 15-(2,5-dimethoxyphenyl)pentadecan-1-ol, the QFA bearing 15 carbon atoms on the side chain (n=15), shows the most potent promotion of axonal growth in the pr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hanbali M,Vela-Ruiz M,Bagnard D,Luu B

更新日期：2006-05-15 00:00:00

abstract：:Group A streptococcus is a Gram-positive bacteria that causes a range of infectious diseases. Targeting the bacteria, a new self-adjuvanting vaccine candidate, incorporating a carbohydrate carrier and an amino acid-based adjuvant, was synthesised utilising carbohydrate chemistry and solid-phase peptide synthesis proce...

journal_title：Bioorganic & medicinal chemistry letters

authors： Simerska P,Lu H,Toth I

更新日期：2009-02-01 00:00:00

abstract：:Several classes of flavonoids (flavones, flavanones, 2'-hydroxychalcones and flavan-4-ols) having a variety of substituents on A ring were investigated for their antiproliferative activity against MCF-7 human breast cancer cells. Structure-activity relationships of these compounds were discussed. 2'-hydroxychalcones a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pouget C,Lauthier F,Simon A,Fagnere C,Basly JP,Delage C,Chulia AJ

更新日期：2001-12-17 00:00:00

abstract：:A series of novel salts made of nicotine alkaloids and bile acids were synthesized and their haemolytic activity was examined in vitro using human erythrocytes. All compounds were characterized by spectroscopic methods. The novel salts show membrane-perturbing properties inducing the erythrocyte shape alterations and ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jasiewicz B,Mrówczyńska L,Malczewska-Jaskóła K

更新日期：2014-02-15 00:00:00

abstract：:Benzylidene-2,4-thiazolidinedione derivatives with substitutions at both the ortho and para-positions of the phenyl group were synthesized as PTP1B inhibitors with IC(50) values in a low micromolar range. Compound 18l, the lowest, bore an IC(50) of 1.3 μM. In a peroxisome proliferator-activated receptor-γ (PPAR-γ) pro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bhattarai BR,Kafle B,Hwang JS,Ham SW,Lee KH,Park H,Han IO,Cho H

更新日期：2010-11-15 00:00:00

abstract：:A low level of high density lipoprotein (HDL) is an independent risk factor for cardiovascular disease. HDL reduces inflammation and plays a central role in reverse cholesterol transport, where cholesterol is removed from peripheral tissues and atherosclerotic plaque. One approach to increase plasma HDL is through inh...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim SH,Johnson JA,Jiang J,Parkhurst B,Phillips M,Pi Z,Qiao JX,Tora G,Ye Chen A,Liu E,Yin X,Yang R,Zhao L,Taylor DS,Basso M,Behnia K,Onorato J,Chen XQ,Abell LM,Lu H,Locke G,Caporuscio C,Adam LP,Gordon D,Wex

更新日期：2019-08-01 00:00:00

abstract：:A photoresponsive RNA aptamer to hemin was selected in vitro from a random sequence library of RNAs with azobenzene residues. The aptamer bound to hemin under visible light irradiation and was released by ultraviolet light. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu M,Jinmei H,Abe H,Ito Y

更新日期：2010-05-01 00:00:00

abstract：:Cyclopenta[g]quinazoline-based inhibitors of thymidylate synthase (TS) possess a chiral centre at the 6-position of the molecule. The effect of this chirality on the inhibition of TS was investigated by synthesising compounds 6S-1a-c, 6R-1a-c. It was shown, in particular with the diastereoisomers 6S-1c, 6R-1c, that th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bavetsias V,Marriott JH,Theti DS,Melin JC,Wilson SC,Jackman AL

更新日期：2001-12-03 00:00:00

abstract：:Seventy-two novel 1,3,4-oxadiazole thioether derivatives containing different flexible-chain moieties were designed and synthesized. The nematicidal activities of all the title compounds were evaluated, and some compounds showed excellent nematicidal activities against citrus nematodes. The compounds 15, 16, 18, 27, 4...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen J,Wei C,Wu S,Luo Y,Wu R,Hu D,Song B

更新日期：2020-04-15 00:00:00

abstract：:Two series of aminosubstituted coumarins were synthesised and evaluated in vitro as inhibitors of DNA gyrase and as potential antibacterials. Novel novobiocin-like coumarins, 4-(dialkylamino)methylcoumarins and 4-((2-alkylamino)ethoxy)coumarins, were discovered as gyrase B inhibitors with promising antibacterial activ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Laurin P,Ferroud D,Schio L,Klich M,Dupuis-Hamelin C,Mauvais P,Lassaigne P,Bonnefoy A,Musicki B

更新日期：1999-10-04 00:00:00

abstract：:The proprotein convertases PCSK8 and PCSK4 are, respectively, the 8th and 4th members of Ca(+2)-dependent serine endoprotease of Proprotein Convertase Subtilisin Kexin (PCSK) super family structurally related to the bacterial subtilisin and yeast kexin. The membrane bound PCSK8 (also called SKI-1 or S1P) is implicated...

journal_title：Bioorganic & medicinal chemistry letters

authors： Basak A,Goswami M,Rajkumar A,Mitra T,Majumdar S,O'Reilly P,Bdour HM,Trudeau VL,Basak A

更新日期：2015-01-01 00:00:00

abstract：:Talaromyces stipitatus ATCC 10500 possesses 17 non-reducing polyketide synthase (NR-PKS) genes. During the course of our functional analysis of PKS genes with a C-terminus methyltransferase domain from T. stipitatus, we expressed tspks2, tspks3 and tspks4 genes in the heterologous host Aspergillus oryzae, respectively...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hashimoto M,Wakana D,Ueda M,Kobayashi D,Goda Y,Fujii I

更新日期：2015-04-01 00:00:00

abstract：:The recent success of vemurafenib shows the importance of selective BRAF V600E inhibition in melanoma. However, paradoxical activation by structurally diverse ATP-competitive RAF kinase inhibitors strongly suggests that selective CRAF inhibitors, not BRAF inhibitors, would be ideal for some Ras mutation cancer treatme...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aman W,Lee J,Kim M,Yang S,Jung H,Hah JM

更新日期：2016-02-15 00:00:00

abstract：:Ligand-based virtual screening led to the discovery of a new class of potent inverse agonists of the human cannabinoid receptor 1, hCB(1), which are selective versus hCB(2). These CB(1) ligands present intriguing departures from a classical CB(1) antagonist pharmacophore. Elements of SAR are discussed in this context....

journal_title：Bioorganic & medicinal chemistry letters

authors： Foloppe N,Allen NH,Bentley CH,Brooks TD,Kennett G,Knight AR,Leonardi S,Misra A,Monck NJ,Sellwood DM

更新日期：2008-02-01 00:00:00

abstract：:A new glucuronylated prodrug of nornitrogen mustard, incorporating the same spacer group as the doxorubicin prodrug HMR 1826, has been prepared. Upon exposure to E. coli beta-glucuronidase, fast hydrolysis occurs but a lower cytotoxicity against LoVo cancer cells is observed compared to the nornitrogen mustard alone. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Papot S,Combaud D,Bosslet K,Gerken M,Czech J,Gesson JP

更新日期：2000-08-21 00:00:00

abstract：:Potent and selective antagonists of the adenosine A2A receptor often contain a nitrogen-rich fused-ring heterocyclic core. Replacement of the core with an isomeric ring system has previously been shown to improve target affinity, selectivity, and in vivo activity. This paper describes the preparation, by a novel route...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dowling JE,Vessels JT,Haque S,Chang HX,van Vloten K,Kumaravel G,Engber T,Jin X,Phadke D,Wang J,Ayyub E,Petter RC

更新日期：2005-11-01 00:00:00