Synthesis and structure-activity relationships of bengazole A analogs.

abstract：:Telomeric G-rich single-stranded DNA can adopt a G-tetraplex structure which has been shown to inhibit telomerase activity. We have examined benzoindoloquinolines derivatives for their ability to stabilize an intramolecular G-quadruplex. The increase in T(m) value of the G-quadruplex was associated with telomerase inh...

journal_title：Bioorganic & medicinal chemistry letters

authors： Alberti P,Schmitt P,Nguyen CH,Rivalle C,Hoarau M,Grierson DS,Mergny JL

更新日期：2002-04-08 00:00:00

abstract：:A novel series of 4-arylphthalazin-1(2H)-one linked to arylpiperidines were synthesized and evaluated as MCH-R1 antagonists. The results of an extensive SAR study probing the effects of substituents on the 4-arylphthalazin-1(2H)-one C-4 aryl group led to the identification of the 4-(3,4-difluorophenyl) derivative as a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lim CJ,Kim SH,Lee BH,Oh KS,Yi KY

更新日期：2012-01-01 00:00:00

abstract：:Retinoid X Receptor (RXR) specific ligands are currently being investigated for the treatment of metabolic diseases such as type II diabetes. We report the synthesis of conformationally locked retinoids, which are potent RXR selective ligands, and the attempted synthesis of 9-cyclopropyl locked analogs of RA and 9-cis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vuligonda V,Garst ME,Chandraratna RA

更新日期：1999-02-22 00:00:00

abstract：:A computer-aided drug design strategy leads to the identification of a new class of p38 inhibitors based on the 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) scaffold. The tolyl triazole amides provided a potent platform amenable to optimization. Further exploration leads to compounds with greater than 100-fold improveme...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cogan DA,Aungst R,Breinlinger EC,Fadra T,Goldberg DR,Hao MH,Kroe R,Moss N,Pargellis C,Qian KC,Swinamer AD

更新日期：2008-06-01 00:00:00

abstract：:We have previously reported the essential structure of the opioid κ receptor agonist nalfurafine hydrochloride (TRK-820) for binding to the κ receptor. In the course of this study, we focused on the effect of the substituent at 17-N in nalfurafine on the binding affinity for the κ receptor. The exchange of the 17-N su...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nemoto T,Yamamoto N,Wada N,Harada Y,Tomatsu M,Ishihara M,Hirayama S,Iwai T,Fujii H,Nagase H

更新日期：2013-01-01 00:00:00

abstract：:Nephropathic cystinosis is a rare autosomal recessive disease characterised by raised intracellular levels of the amino acid, cystine. If untreated, the disease, progressively deteriorates towards end stage renal disease (ESRD) at the end of the first decade. The disease is caused by a defect in the lysosomal transpor...

journal_title：Bioorganic & medicinal chemistry letters

authors： Omran Z,Kay G,Hector EE,Knott RM,Cairns D

更新日期：2011-04-15 00:00:00

abstract：:A novel series of aminopyrimidinylisoindoline derivatives 1a-w having an aminopyrimidine scaffold as a hinge region binding motif were designed and synthesized. Among them, six compounds showed potent inhibitory activities against AXL kinase with IC50 values of submicromolar range. Especially, compound 1u possessing (...

journal_title：Bioorganic & medicinal chemistry letters

authors： Choi MJ,Roh EJ,Hur W,Lee SH,Sim T,Oh CH,Lee SH,Kim JS,Yoo KH

更新日期：2018-12-15 00:00:00

abstract：:p38alpha Mitogen Activated Protein Kinase (MAP kinase) is an intracellular soluble serine threonine kinase. p38alpha kinase is activated in response to cellular stresses, growth factors and cytokines such as interleukin-1 (IL-1) and tumor necrosis factor alpha (TNF-alpha). The central role of p38alpha activation in se...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mavunkel BJ,Chakravarty S,Perumattam JJ,Luedtke GR,Liang X,Lim D,Xu YJ,Laney M,Liu DY,Schreiner GF,Lewicki JA,Dugar S

更新日期：2003-09-15 00:00:00

abstract：:Nucleoside transporter inhibitors have potential therapeutic applications as anticancer, antiviral, cardioprotective, and neuroprotective agents. We have synthesized and flow cytometrically evaluated the binding affinity of a series of novel halogenated nitrobenzylthioinosine analogs at the human es nucleoside transpo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gupte A,Buolamwini JK

更新日期：2004-05-03 00:00:00

abstract：:Synthetic array technology was utilized to rapidly synthesize and analyze a diverse set of reductive alkylation analogues of daptomycin. Analysis of the array suggested the use of polar functionality such as sulfonamides or amide or polar spaces such as piperazine would beneficially affect activity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Siedlecki J,Hill J,Parr I,Yu X,Morytko M,Zhang Y,Silverman J,Controneo N,Laganas V,Li T,Li J,Keith D,Shimer G,Finn J

更新日期：2003-12-01 00:00:00

abstract：:By linking the mercapto groups with isopropyl and introducing L-amino acid into the 5-carboxyl of DMSA a class of novel 5-(1-carbonyl-L-amino-acid)-2,2- dimethyl-[1,3]dithiolane-4-carboxylic acids were prepared. Their in vivo activities were evaluated on lead loaded mice at the dose of 0.4 mmol/kg. The results showed ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu Y,Wang Y,Zhao M,Hou B,Peng L,Zheng M,Wu J,Peng S

更新日期：2011-03-15 00:00:00

abstract：:Twenty-five novel pregnenolone/2-cyanoacryloyl conjugates (6-30) were designed and prepared, with the aim of developing novel anticancer drugs with dual NF-κB inhibitory and anti-proliferative activities. Compounds 22 and 27-30 showed inhibition against TNF-α-induced NF-κB activation in luciferase assay, which was con...

journal_title：Bioorganic & medicinal chemistry letters

authors： Song JL,Zhang J,Liu CL,Liu C,Zhu KK,Yang FF,Liu XG,Figueiró Longo JP,Alexandre Muehlmann L,Azevedo RB,Zhang YY,Guo YW,Jiang CS,Zhang H

更新日期：2017-10-15 00:00:00

abstract：:We describe the synthesis and binding affinities on D(2), 5-HT(2A) and 5-HT(2C) receptors of 6-aminomethyl-6,7-dihydro-1H-indazol-4(5H)-ones and 6-aminomethyl-6,7-dihydro-3-methyl-benzo[d]isoxazol-4(5H)-ones, as conformationally constrained butyrophenone analogues. One of the new compounds showed good in vitro binding...

journal_title：Bioorganic & medicinal chemistry letters

authors： Barceló M,Raviña E,Masaguer CF,Domínguez E,Areias FM,Brea J,Loza MI

更新日期：2007-09-01 00:00:00

abstract：:The synthesis and biological evaluation of novel human A-FABP inhibitors based on the 6-(trifluoromethyl)pyrimidine-4(1H)-one scaffold is described. Two series of compounds, bearing either an amino or carbon substituent in the 2-position of the pyrimidine ring were investigated. Modification of substituents and chain ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ringom R,Axen E,Uppenberg J,Lundbäck T,Rondahl L,Barf T

更新日期：2004-09-06 00:00:00

abstract：:Modification of the biphenyl portion of MMP inhibitor 2a gave analogue 2i which is greater than 1000-fold selective against MMP-2 versus MMP-1. The stereospecific synthesis of both enantiomers of 2i was achieved beginning with (S)- or (R)-benzyl glycidyl ether. The (S)-enantiomer, 11 (ABT-770), is orally bioavailable ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Curtin ML,Florjancic AS,Heyman HR,Michaelides MR,Garland RB,Holms JH,Steinman DH,Dellaria JF,Gong J,Wada CK,Guo Y,Elmore IB,Tapang P,Albert DH,Magoc TJ,Marcotte PA,Bouska JJ,Goodfellow CL,Bauch JL,Marsh KC,Morgan

更新日期：2001-06-18 00:00:00

abstract：:Thienylpyrimidines substituted at position 2 of the pyrimidine with a chiral aminoalkoxy group were synthesized. Upon interaction with duplex DNA, the unfused heteroaromatic system of these compounds intercalates with DNA base pairs and the protonated side chain is located in the major groove. The S-enantiomers bind m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Strekowski L,Cegla MT,Honkan V,Buczak H,Winkeljohn WR,Baumstark AL,Wilson WD

更新日期：2005-06-02 00:00:00

abstract：:Novel analogues of the angiotensin I-converting enzyme (ACE) inhibitor keto-ACE were synthesized via a facile Horner-Emmons olefination of a phosphonoketone precursor with ethyl glyoxylate. Introduction of a bulky aromatic tryptophan at the P(2)(') position of keto-ACE resulted in a significant increase in C-domain-se...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nchinda AT,Chibale K,Redelinghuys P,Sturrock ED

更新日期：2006-09-01 00:00:00

abstract：:A series of 6-substituted sulfocoumarins incorporating substituted-1,2,3-triazol-4-yl-/5-yl moieties were synthesized by employing click chemistry. The new sulfocoumarins incorporated cycloalkyl, tert-butyl and substituted aryl moieties at the triazole ring, and were investigated for the inhibition of four human (h) c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Grandane A,Tanc M,Zalubovskis R,Supuran CT

更新日期：2014-03-01 00:00:00

abstract：:3-Trifluoromethylflavonoid derivatives were prepared for the first time by trifluoromethylation of 3-iodoflavonoid derivatives. Other C ring and B ring trifluoromethylated flavonoid derivatives were also prepared. All the compounds were tested for their effect on the U2OS cell cycle in vitro. Bistrifluoromethylated ap...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang CL,Li HQ,Meng WD,Qing FL

更新日期：2005-10-15 00:00:00

abstract：:Regioselective synthesis of a number of highly functionalized 3-benzylpyrimidino chromen-2-ones (4) were accomplished in a one pot three component reaction in acetic acid and determined their anti-microbial and anti-biofilm activities. Compounds 4o and 4p showed an excellent anti-microbial activity against Micrococcus...

journal_title：Bioorganic & medicinal chemistry letters

authors： Emmadi NR,Atmakur K,Bingi C,Godumagadda NR,Chityal GK,Nanubolu JB

更新日期：2014-01-15 00:00:00

abstract：:An asymmetric synthesis of alpha-amino acids with novel beta-branched side chains has been implemented. The syntheses feature a p-toluenesulfinylimine induced chiral Strecker approach and were found to be applicable to the introduction of both aliphatic and aromatic beta-branched sidechains for preparation of previous...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang M,Porte A,Diamantidis G,Sogi K,Kubrak D,Resnick L,Mayer SC,Wang Z,Kreft AF,Harrison BL

更新日期：2007-05-01 00:00:00

abstract：:Urea-based inhibitors of human glutamate carboxypeptidase II (GCPII) have advanced into clinical trials for imaging metastatic prostate cancer. In parallel efforts, agents with increased lipophilicity have been designed and evaluated for targeting GCPII residing within the neuraxis. Here we report the structural and c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pavlicek J,Ptacek J,Cerny J,Byun Y,Skultetyova L,Pomper MG,Lubkowski J,Barinka C

更新日期：2014-05-15 00:00:00

abstract：:Poor prognosis coupled with significant economic burden makes heart failure (HF) one of the largest issues currently facing the world population. Although a significant number of new therapies have emerged over the past 20 years to treat the underlying physiological risk factors, only two new medications specifically ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Malinowski JT,St Jean DJ Jr

更新日期：2018-05-15 00:00:00

abstract：:A MeOH extract of the dry root of Lithospermum erythrorhizon showed strong increasing effect on serine palmitoyltransferase (SPT) in normal human keratinocyte cells (HaCaT cells). Bioassay-guided separation on this extract using repeated chromatography resulted in the isolation of lithospermic acid (1) and two derivat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thuong PT,Kang KW,Kim JK,Seo DB,Lee SJ,Kim SH,Oh WK

更新日期：2009-03-15 00:00:00

abstract：:The our previous study synthesized the chrysin-chromene-spirooxindole hybrids 3, and further found compound 3e had good antitumor activity against A549 cells in vitro through multi-target co-regulation of the p53 signalling pathway to inhibit the proliferation of A549 cells. This study was designed to evaluate the ant...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang WH,Chen S,Liu XL,Bing-Lin,Liu XW,Zhou Y

更新日期：2020-09-01 00:00:00

abstract：:The discovery and optimization of novel pyrrolo[3,4-b]pyridin-7(6H)-one MCH-R1 antagonists are described. A systematic SAR study probing the effects of aryl-, benzyl- and arylthio-substituents at the 2-position of the pyrrolo[3,4-b]pyridin-7(6H)-ones led to identification of the 2-[(4-fluorophenyl)thio] derivative 7b ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lim CJ,Kim JY,Lee BH,Oh KS,Yi KY

更新日期：2013-03-15 00:00:00

abstract：:Three new (1-3) and one known (4) bioactive terpenoids were isolated from the seeds of Silybum marianum based on the investigation to get new NO inhibitors. Their structures were determined by extensive NMR (1D and 2D NMR) and MS spectroscopic data, and the absolute configurations were identified by experimental and c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qin NB,Li SG,Yang XY,Gong C,Zhang XY,Wang J,Li DH,Guo YQ,Li ZL,Hua HM

更新日期：2017-05-15 00:00:00

abstract：:A series of artemisinin derived esters 7a-j, incorporating pharmacologically privileged substructure, such as biphenyl, adamantane and fluorene, have been prepared and evaluated for antimalarial activity against multidrug-resistant (MDR) Plasmodium yoelii nigeriensis by oral route. Several of these compounds were foun...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh C,Chaudhary S,Puri SK

更新日期：2008-02-15 00:00:00

abstract：:Our series of competitive antagonists against the G-protein coupled receptor P2Y(14) were found to be highly shifted in the presence of serum (>99% protein bound). A binding assay using 2% human serum albumin (HSA) was developed to guide further SAR studies and led to the identification of the zwitterion 2, which is s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Robichaud J,Fournier JF,Gagné S,Gauthier JY,Hamel M,Han Y,Hénault M,Kargman S,Levesque JF,Mamane Y,Mancini J,Morin N,Mulrooney E,Wu J,Black WC

更新日期：2011-07-15 00:00:00

abstract：:Eight monosaccharide analogs of the potent antitumor OSW saponins (2-9) were synthesized. One analog, 2-O-acetyl-alpha-l-arabinopyranoside 3, showed antiproliferative activity against the Jurkat cells (IC(50)=0.078microM) comparable to that of the disaccharide derivative (1). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tang P,Mamdani F,Hu X,Liu JO,Yu B

更新日期：2007-02-15 00:00:00