Vialinin A and thelephantin G, potent inhibitors of tumor necrosis factor-α production, inhibit sentrin/SUMO-specific protease 1 enzymatic activity.

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：:ADX88178 (1) has been recently developed as a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4). The aim of this study was to develop [(11)C]1 as a novel positron emission tomography ligand and to evaluate its binding ability for mGluR4. Using stannyl precursor 3, [(11)C]1 was efficie...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fujinaga M,Yamasaki T,Nengaki N,Ogawa M,Kumata K,Shimoda Y,Yui J,Xie L,Zhang Y,Kawamura K,Zhang MR

更新日期：2016-01-15 00:00:00

abstract：:We designed and synthesized a small series of 2-aryl-imidazo[2,1-b]benzothiazole, representing a combination of motifs from the two most potent amyloid imaging agents, PIB and IMPY. The binding affinity of the new compounds ranged from 6 to 133 nM. Among the best compounds, 3b (K(i)=6 nM) can be labeled with (11)CH(3)...

journal_title：Bioorganic & medicinal chemistry letters

authors： Alagille D,DaCosta H,Baldwin RM,Tamagnan GD

更新日期：2011-05-15 00:00:00

abstract：:A tetrahydropyran-based inhibitor (2) of mammalian ribonucleotide reductase (mRR) has been designed and synthesized based on the heptapeptide, N-AcFTLDADF (1), corresponding to the C-terminus of the R2 subunit of mRR. Inhibition studies revealed that 2 is indeed a competent inhibitor, albeit less potent than 1. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Smith AB 3rd,Sasho S,Barwis BA,Sprengeler P,Barbosa J,Hirschmann R,Cooperman BS

更新日期：1998-11-17 00:00:00

abstract：:In the catalytic core of 10-23 DNAzyme, its five adenine residues are moderate conservative, but with highly conserved functional groups like 6-amino group and 7-nitrogen atom. It is this critical conservation that these two groups could be modified for better contribution. With 2'-deoxyadenosine analogues, several fu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhu J,Li Z,Wang Q,Liu Y,He J

更新日期：2016-09-15 00:00:00

abstract：:A concise synthesis of three novel C2-C3 unsaturated pyrrolo[2,1-c][1,4]benzodiazepine analogues (18-20) containing conjugated acrylyl C2-substituents is reported that utilises Heck coupling to install the C2-acrylyl side chains. These analogues possess significant cytotoxicity according to the NCI 60-cell line screen...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen Z,Gregson SJ,Howard PW,Thurston DE

更新日期：2004-03-22 00:00:00

abstract：:The (S,S,S,R,S,R)-configurated cyclohexadepsipeptides (CHDPs) represent novel enniatin derivatives with strong in vivo activity against the parasitic nematode Haemonchus contortus Rudolphi in sheep. 2D NMR spectroscopic analysis revealed for the major conformation the asymmetric conformer, containing a cis-amide bond ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jeschke P,Benet-Buchholz J,Harder A,Etzel W,Schindler M,Thielking G

更新日期：2003-10-06 00:00:00

abstract：:GTP cyclohydrolase (GCYH-I) is an enzyme in the folate biosynthesis pathway that has not been previously exploited as an antibiotic target, although several pathogens including N. gonorrhoeae use a form of the enzyme GCYH-IB that is structurally distinct from the human homologue GCYH-IA. A comparison of the crystal st...

journal_title：Bioorganic & medicinal chemistry letters

authors： Samaan GN,Paranagama N,Haque A,Hecht DA,Swairjo MA,Purse BW

更新日期：2020-01-15 00:00:00

abstract：:4,7-Dichloro-1-benzothien-2-yl sulfonylaminomethyl boronic acid (DSABA, Compound I) was discovered as the first boronic acid-based class D beta-lactamase inhibitor. It exhibited an IC(50) of 5.6 microM against OXA-40. The compound also inhibited class A and C beta-lactamases with sub to low microM IC(50), and synergiz...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tan Q,Ogawa AM,Painter RE,Park YW,Young K,DiNinno FP

更新日期：2010-04-15 00:00:00

abstract：:The continual increase in drug resistance; the lack of new chemotherapeutic agents; the toxicity of existing agents and the increasing morbidity with HIV co-infection mean the search for new antileishmanial agents has never been more urgent. We have identified the benzodiazepines as a structural class for antileishman...

journal_title：Bioorganic & medicinal chemistry letters

authors： Clark RL,Carter KC,Mullen AB,Coxon GD,Owusu-Dapaah G,McFarlane E,Duong Thi MD,Grant MH,Tettey JN,Mackay SP

更新日期：2007-02-01 00:00:00

abstract：:New analogues of the previously described 3-aryl pyridone KOR agonists have been synthesised by parallel synthetic methods, both in solution- and with solid-phase chemistry, making use of the well known and versatile Mitsunobu, Suzuki and Buchwald reactions. Opioid receptor binding data for the compounds produced is r...

journal_title：Bioorganic & medicinal chemistry letters

authors： Semple G,Andersson BM,Chhajlani V,Georgsson J,Johansson MJ,Rosenquist A,Swanson L

更新日期：2003-03-24 00:00:00

abstract：:4-(Substituted-benzylidine)-2-substituted-5,6-dihydrobenzo[h]quinazoline (5a-p) and 4-(substituted-benzylidine)-2-substituted-3, 4, 5, 6-tetrahydrobenzo[h]quinazoline (6a-p) have been synthesized from 2-(substituted-benzylidine)tetralone-1(3a-d) and several substituted guanidine sulfates(4a-d).These compounds were tes...

journal_title：Bioorganic & medicinal chemistry letters

authors： Agarwal KC,Sharma V,Shakya N,Gupta S

更新日期：2009-09-15 00:00:00

abstract：:Compounds based on the 2,3-distyrylindole scaffold were found to exhibit bactericidal properties upon irradiation with white light. At the concentration of 1 μM, the lead compound 1 completely (ca. 109 CFU/mL) eradicated such Gram-positive organisms as S. aureus (MRSA, MSSA), E. faecalis (VRE), S. pyogenes and S. muta...

journal_title：Bioorganic & medicinal chemistry letters

authors： Edwards L,Turner D,Champion C,Khandelwal M,Zingler K,Stone C,Rajapaksha RD,Yang J,Ranasinghe MI,Kornienko A,Frolova LV,Rogelj S

更新日期：2018-06-01 00:00:00

abstract：:5-(2,8-Bis(trifluoromethyl)quinolin-4-yloxymethyl)isoxazole-3-carboxylic acid ethyl ester (compound 3) was reported to have excellent antituberculosis activity against both replicating and non-replicating Mycobacterium tuberculosis, with a minimum inhibitory concentration (MIC) of 0.9 microM and 12.2 microM, respectiv...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mao J,Yuan H,Wang Y,Wan B,Pak D,He R,Franzblau SG

更新日期：2010-02-01 00:00:00

abstract：:The carbodiimides 2, obtained from aza-Wittig reactions of iminophosphorane 1 with aromatic isocyanates, reacted with ammonia to give ethyl 3,4-dihydro-6-methyl-4-oxo-2-arylamino-furo[2,3-d]pyrimidine-5-carboxylate 3. Further reaction of 3 with POCl(3) and various amines generated ethyl 4-alkylamino-2-arylamino-6-meth...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hu YG,Wang Y,Du SM,Chen XB,Ding MW

更新日期：2010-11-01 00:00:00

abstract：:Docking studies of 4-phenylthiazolinethione on human IDO1 suggest complexation of the heme iron by the exocyclic sulfur atom further reinforced by hydrophobic interactions of the phenyl ring within pocket A of the enzyme. On this basis, chemical modifications were proposed to increase inhibition activity. Synthetic ro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Balti M,Plas A,Meinguet C,Haufroid M,Thémans Q,Efrit ML,Wouters J,Lanners S

更新日期：2017-08-01 00:00:00

abstract：:The design and synthesis of a novel series of non-nucleoside HIV reverse transcriptase inhibitors (NNRTIs) based on a pyrazole template is described. These compounds are active against wild type reverse transcriptase (RT) and retain activity against clinically important mutants. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mowbray CE,Burt C,Corbau R,Perros M,Tran I,Stupple PA,Webster R,Wood A

更新日期：2009-10-01 00:00:00

abstract：:A group of sixteen iridoids isolated from plants used as anti-inflammatory remedies in Mexican folk medicine were evaluated for their potential to inhibit cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes. From these assays, loganic acid (10) was identified as the most promising compound with both COX-1 (3...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ramírez-Cisneros MÁ,Rios MY,Aguilar-Guadarrama AB,Rao PP,Aburto-Amar R,Rodríguez-López V

更新日期：2015-10-15 00:00:00

abstract：:Structural features from the anticancer prodrug nemorubicin (MMDX) and the DNA-binding molecule DRAQ5™ were used to prepare anthraquinone-based compounds, which were assessed for their potential to interrogate cytochrome P450 (CYP) functional activity and localisation. 1,4-disubstituted anthraquinone 8 was shown to be...

journal_title：Bioorganic & medicinal chemistry letters

authors： Errington RJ,Sadiq M,Cosentino L,Wiltshire M,Sadiq O,Sini M,Lizano E,Pujol MD,Morais GR,Pors K

更新日期：2018-05-01 00:00:00

abstract：:3-O-tert-Butyldimethylsilyl-17 alpha-(6-mesyloxyhexynyl)estradiol was converted to the azide in 60-70% yield with NaN3/DMPU, then reduced to the corresponding amine (> 95% yield). Acylation with the N-hydroxysuccinimide esters of biotin, 5-carboxyfluorescein and 10-(3-sulfopropyl)-N-tosyl-N-(3- carboxypropyl)acridiniu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Adamczyk M,Chen YY,Moore JA,Mattingly PG

更新日期：1998-06-02 00:00:00

abstract：:During development of nitroheterocycles with potential antimycobacterial activities we have tested against Mycobacterium tuberculosis a number of pyrroles strictly related to pyrrolnitrin, an antifungal antibiotic isolated from Streptomyces pyrrocinia. Some of the tested arylpyrrole derivatives and pyrrolnitrin have s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Di Santo R,Costi R,Artico M,Massa S,Lampis G,Deidda D,Pompei R

更新日期：1998-10-20 00:00:00

abstract：:Ganglioside GM1 mimics including (R)-2-hydroxy-3-cyclohexylpropionic acid or (R)-2-hydroxy-3-phenylpropionic acid as replacements for NeuAc are stronger cholera toxin binders than the parent ligand 2, which includes (R)-2-hydroxy-propionic acid. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Arosio D,Baretti S,Cattaldo S,Potenza D,Bernardi A

更新日期：2003-11-03 00:00:00

abstract：:Dysregulation of cell signalling processes caused by an enhanced activity of protein kinases mainly contributes to cancer progression. Protein kinase inhibitors have been established as promising drugs that inhibit such overactive protein kinases in cancer cells. The formation of metastases, which makes a therapy diff...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mahmoud KA,Krug M,Wersig T,Slynko I,Schächtele C,Totzke F,Sippl W,Hilgeroth A

更新日期：2014-04-15 00:00:00

abstract：:The synthesis and biological evaluation of a series of novel isobenzofuran-based compounds are described. The compounds were evaluated for their immunosuppressive effects of T-cell proliferation and IMPDH type II inhibitor activity in vitro, as well as their structure-activity relationships were assessed. Several comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang N,Wang QH,Wang WQ,Wang J,Li F,Tan SP,Cheng MS

更新日期：2012-01-01 00:00:00

abstract：:A series of 4-aryl-3-aminoquinoline-2-one derivatives was synthesized and evaluated as activators of the cloned maxi-K channel mSlo (hSlo) expressed in Xenopus laevis oocytes using electrophysiological methods. A brain penetrable activator of maxi-K channels was identified and shown to be significantly active in the M...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hewawasam P,Fan W,Knipe J,Moon SL,Boissard CG,Gribkoff VK,Starrett JE

更新日期：2002-07-08 00:00:00

abstract：:Naturally occurring flavonoids co-exist as glycoside conjugates, which dominate aglycones in their content. To unveil the structure-activity relationship of a naturally occurring flavonoid, we investigated the effects of the glycosylation of naringenin on the inhibition of enzyme systems related to diabetes (protein t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jung HA,Paudel P,Seong SH,Min BS,Choi JS

更新日期：2017-06-01 00:00:00

abstract：:An HTS campaign of our corporate compound library resulted in thieno[2,3-b]pyridines derivative hits with mGluR5 negative allosteric modulator effects. During the hit-to-lead development our objective was to improve affinity, and to keep the ligand efficiency values at an acceptable level. After different modification...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nógrádi K,Wágner G,Domány G,Bobok A,Magdó I,Kiss B,Kolok S,Fónagy K,Gyertyán I,Háda V,Kóti J,Gál K,Farkas S,Keserű GM,Greiner I,Szombathelyi Z

更新日期：2014-08-15 00:00:00

abstract：:A thiazolidine-2,4-dione derivative, 3-(2-aminoethyl)-5-(3-phenyl-propylidene)-thiazolidine-2,4-dione (2), was identified as a dual inhibitor of the Raf/MEK/ extracellular signal-regulated kinase (ERK) and the phosphatidylinositol 3-kinase (PI3K)/Akt signaling cascades. The discovered compound inhibited cell prolifera...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li Q,Wu J,Zheng H,Liu K,Guo TL,Liu Y,Eblen ST,Grant S,Zhang S

更新日期：2010-08-01 00:00:00

abstract：:The convergent synthesis of C35-fluorinated analogues of solamin, a mono-THF Annonaceous acetogenin, has been achieved by the Sonogashira coupling of the THF ring fragment and the fluorinated γ-lactone fragment. It was revealed that the number of fluorine atoms on the γ-lactone moiety affects the growth inhibitory act...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kojima N,Suga Y,Hayashi H,Yamori T,Yoshimitsu T,Tanaka T

更新日期：2011-10-01 00:00:00

abstract：:A novel series of aminopyrimidine IKK2 inhibitors have been developed which show excellent in vitro inhibition of this enzyme and good selectivity over the IKK1 isoform. The relative potency and selectivity of these compounds has been rationalized using QSAR and structure-based modelling. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bingham AH,Davenport RJ,Gowers L,Knight RL,Lowe C,Owen DA,Parry DM,Pitt WR

更新日期：2004-01-19 00:00:00