Ritonavir-boosted indinavir but not lopinavir inhibits erythrocytic stage Plasmodium knowlesi malaria in rhesus macaques.

abstract：:A catalyst-free synthesis of 6,9-dihydro-[1,3]dioxolo[4,5-g]thieno[3,4-b]quinolin-8(5H)-ones as novel analogues of podophyllotoxins was developed by a three-component reaction of aldehydes, ethyl 2,4-dioxotetrahydrothiophene-3-carboxylate and 3,4-(methylenedioxy)aniline. This methodology not only provides new chemical...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li T,Lu T,Yu C,Yao C

更新日期：2015-04-01 00:00:00

abstract：:A series of 1-aryl-6,7-dihydroxyl(methoxy)-1,2,3,4-tetrahydroisoquinolines (compounds 1-36) were synthesized via Pictet-Spengler cyclization. All the synthesized compounds were assayed for activities against HIV-1(IIIB) in C8166 cell cultures by MTT method for the first time. The results of the anti-HIV screening reve...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cheng P,Huang N,Jiang ZY,Zhang Q,Zheng YT,Chen JJ,Zhang XM,Ma YB

更新日期：2008-04-01 00:00:00

abstract：:Analysis of the enantiomers of rosiglitazone in a PPAR gamma binding assay suggests that the (S)-(-)-isomer is responsible for the antidiabetic activity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Parks DJ,Tomkinson NC,Villeneuve MS,Blanchard SG,Willson TM

更新日期：1998-12-15 00:00:00

abstract：:By developing a new synthetic procedure for introduction of side chains onto the camptothecin ring system, we were able to achieve the preparation of a number of analogs bearing bulky, hydrophobic groups directly attached to the 7-position. These include 7-tert-butylcamptothecin, 7-benzylcamptothecin and the correspon...

journal_title：Bioorganic & medicinal chemistry letters

authors： Manikumar G,Wadkins RM,Bearss D,Von Hoff DD,Wani MC,Wall ME

更新日期：2004-11-01 00:00:00

abstract：:Benzalacetone synthase (BAS) and chalcone synthase (CHS) are plant-specific type III polyketide synthases (PKSs), sharing 70% amino acid sequence identity and highly homologous overall protein structures. BAS catalyzes the decarboxylative coupling of 4-coumaroyl-CoA with malonyl-CoA to produce the diketide benzalaceto...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shimokawa Y,Morita H,Abe I

更新日期：2010-09-01 00:00:00

abstract：:A series of 7-acyloxymethylcamptothecin and 20-O-acyl-7-acyloxymethylcamptothecin derivatives were regioselectively prepared on different solvents. 7-Acyloxymethylcamptothecins possess more efficacy than 20-O-acyl-7-acyloxymethylcamptothecins against six human cancer cell lines in vitro. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pan XD,Han R,Sun PY

更新日期：2003-11-03 00:00:00

abstract：:Using a phenotypic screening and SAR optimization approach, a phenyl-bis-oxazole derivative has been identified with anti-proliferative activity, optimized with the use of a panel of cancer cell lines. The lead compound was synthesized by means of a short and effective two-step synthesis using Pd-catalyzed direct aryl...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ohnmacht SA,Ciancimino C,Vignaroli G,Gunaratnam M,Neidle S

更新日期：2013-10-01 00:00:00

abstract：:Benzylamides of pentanedioic acid were identified as inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) by high-throughput screening. Optimisation to 2-adamantyl amides yielded inhibitors with single digit nanomolar IC(50)s on the 11beta-HSD1 human isoform. The hydroxy adamantyl amide lead compound...

journal_title：Bioorganic & medicinal chemistry letters

authors： Roche D,Carniato D,Leriche C,Lepifre F,Christmann-Franck S,Graedler U,Charon C,Bozec S,Doare L,Schmidlin F,Lecomte M,Valeur E

更新日期：2009-05-15 00:00:00

abstract：:C-6 Biarylmethylamino purine derivatives of roscovitine (1) inhibit cyclin dependent kinases and demonstrate potent antiproliferative activity. Replacement of the aryl rings of the C-6 biarylmethylamino group with heterobiaryl rings has provided compounds with significantly improved activity. In particular, derivative...

journal_title：Bioorganic & medicinal chemistry letters

authors： Trova MP,Barnes KD,Alicea L,Benanti T,Bielaska M,Bilotta J,Bliss B,Duong TN,Haydar S,Herr RJ,Hui Y,Johnson M,Lehman JM,Peace D,Rainka M,Snider P,Salamone S,Tregay S,Zheng X,Friedrich TD

更新日期：2009-12-01 00:00:00

abstract：:Non-nucleoside inhibitors of HIV-1 reverse transcriptase are reported that have ca. 100-fold greater solubility than the structurally related drugs etravirine and rilpivirine, while retaining high anti-viral activity. The solubility enhancements come from strategic placement of a morpholinylalkoxy substituent in the e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bollini M,Cisneros JA,Spasov KA,Anderson KS,Jorgensen WL

更新日期：2013-09-15 00:00:00

abstract：:Eight esters of 2-(1-hydroxyalkyl)-1,4-dihydroxy-9,10-anthraquinone with melphalan were prepared and tested for their antitumor activity (S-180) and cytotoxicity. 2-[1-[4-(p-Bis(2-chloroethyl)-aminophenyl)-butanoyloxy]methyl]-1,4-dihydroxy-9,10-anthraquinone and 2-[1-[4-(p-bis(2-chloroethyl)-aminophenyl)-butanoyloxy]e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jin G,You Y,Ahn B

更新日期：2001-06-04 00:00:00

abstract：:Structure-guided design led to the discovery of novel chemical scaffolds for B-Raf inhibitors. Both type I and type II kinase inhibitors have been explored and lead compounds with good potency and excellent selectivity have been identified. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang X,Salaski EJ,Berger DM,Powell D,Hu Y,Wojciechowicz D,Collins K,Frommer E

更新日期：2011-12-01 00:00:00

abstract：:A new series of 2-(benzyloxy)benzamides are presented that are potent functional antagonists of TRPM8 and possess improved LipE and LE compared to the original lead. They were discovered through a series of compound libraries and we present a powerful visualization method for the chemical space explored with each libr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Brown A,Ellis D,Favor DA,Kirkup T,Klute W,MacKenny M,McMurray G,Stennett A

更新日期：2013-11-15 00:00:00

abstract：:We report the results of our study into a series of simple phenyl and alkyl sulfamates and alkyl methanesulfonates as potential inhibitors of the enzyme estrone sulfatase (ES). The results of the study show that the substituted phenyl sulfamates are good irreversible inhibitors; the alkyl sulfamate compounds were foun...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ahmed S,James K,Owen CP,Patel CK,Sampson L

更新日期：2002-05-06 00:00:00

abstract：:Poly(ADP-ribose)polymerase-I (PARP-1) enzyme is involved in maintaining DNA integrity and programmed cell death. A virtual screening of commercial libraries led to the identification of five novel scaffolds with inhibitory profile in the low nanomolar range. A hit-to-lead optimization led to the identification of a gr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Giannini G,Battistuzzi G,Vesci L,Milazzo FM,De Paolis F,Barbarino M,Guglielmi MB,Carollo V,Gallo G,Artali R,Dallavalle S

更新日期：2014-01-15 00:00:00

abstract：:Based on the favorable antiviral profiles of 4'-substituted nucleosides, novel 1-(2'-deoxy-2'-fluoro-4'-C-ethynyl-beta-D-arabinofuranosyl)-uracil (1a), -thymine (1b), and -cytosine (2) analogs were synthesized. Compounds 1b and 2 exhibited potent anti-HIV-1 activity with IC(50) values of 86 and 1.34 nM, respectively, ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang Q,Li Y,Song C,Qian K,Chen CH,Lee KH,Chang J

更新日期：2010-07-15 00:00:00

abstract：:Four novel mononuclear complexes, [Cd(L)2·2H2O] (1), [Ni(L)2·2H2O] (2) [Cu(L)2·H2O] (3), and [Zn(L)2·2H2O] (4) (CCDC numbers: 1444630-1444633 for complexes 1-4) (HL=4-(2,3-dichlorophenyl)piperazine-1-carboxylic acid) were synthesized, and have been characterized by IR spectroscopy, elemental analysis, and X-ray crysta...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang DD,Chen YN,Wu YS,Wang R,Chen ZJ,Qin J,Qian SS,Zhu HL

更新日期：2016-07-15 00:00:00

abstract：:The design and profile of a series of adamantyl-containing long acting beta(2)-adrenoreceptor agonists are described. An optimal pharmacokinetic profile of low oral bioavailability was combined with a strong pharmacology profile when assessed using a guinea pig trachea tissue model. A focus was then placed on developi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Brown AD,Bunnage ME,Glossop PA,James K,Jones R,Lane CA,Lewthwaite RA,Mantell S,Perros-Huguet C,Price DA,Trevethick M,Webster R

更新日期：2008-02-15 00:00:00

abstract：:Cyclic peptides were obtained, on-resin, by the copper (I) catalysed 1,3-dipolar cycloaddition of azides and alkynes. The reaction led exclusively to the formation of the expected cyclomonomeric products which acted as ligands of the Vascular Endothelial Growth Factor receptor 1. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Goncalves V,Gautier B,Regazzetti A,Coric P,Bouaziz S,Garbay C,Vidal M,Inguimbert N

更新日期：2007-10-15 00:00:00

abstract：:A series of CCR5 antagonists were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, potency shift in the presence of α-glycoprotein were evaluated in rat and dog pharmacokinetics. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Skerlj R,Bridger G,Zhou Y,Bourque E,McEachern E,Langille J,Harwig C,Veale D,Yang W,Li T,Zhu Y,Bey M,Baird I,Sartori M,Metz M,Mosi R,Nelson K,Bodart V,Wong R,Fricker S,Mac Farland R,Huskens D,Schols D

更新日期：2011-12-01 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 series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, was synthesized and evaluated. The most potent compound in this series, compound 7, structurally resembles the potent anti-microtubule agent Combretastatin A-4, inhibited tubulin polymerizat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li PK,Xiao Z,Hu Z,Pandit B,Sun Y,Sackett DL,Werbovetz K,Lewis A,Johnsamuel J

更新日期：2005-12-15 00:00:00

abstract：:Quantitative fluorescence-based methods have been developed to determine the nuclear concentration of polyamide-fluorescein conjugates in cell culture. Confocal laser scanning microscopy and flow cytometry techniques are utilized to plot calibration curves, from which the nuclear concentration can be interpolated. Upo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hsu CF,Dervan PB

更新日期：2008-11-15 00:00:00

abstract：:Human isoprenylcysteine carboxyl methyltransferase (hIcmt) is a promising anticancer target as it is important for the post-translational modification of oncogenic Ras proteins. We herein report the synthesis and biochemical activity of 41 farnesyl-cysteine based analogs versus hIcmt. We have demonstrated that the ami...

journal_title：Bioorganic & medicinal chemistry letters

authors： Majmudar JD,Hahne K,Hrycyna CA,Gibbs RA

更新日期：2011-05-01 00:00:00

abstract：:MDM2 and MDMX are oncoproteins that negatively regulate the activity and stability of the tumor suppressor protein p53. The inhibitors of protein-protein interactions (PPIs) of MDM2-p53 and MDMX-p53 represent potential anticancer agents. In this study, a novel approach for identifying MDM2-p53 and MDMX-p53 PPI inhibit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Noguchi T,Oishi S,Honda K,Kondoh Y,Saito T,Kubo T,Kaneda M,Ohno H,Osada H,Fujii N

更新日期：2013-07-01 00:00:00

abstract：:A group of (Z)-1,2-diphenyl-1-[4-[2-(4-methylpiperazin-1-yl)ethoxy]phenyl]but-1-enes were synthesized using methodologies that will allow incorporation of a [(124)I]iodine substituent at the para-position of either the C-1 phenyl ring or the C-2 phenyl ring, or a [(18)F]OCH(2)CH(2)F substituent at the para-position of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Abdellatif KR,Velázquez CA,Huang Z,Chowdhury MA,Knaus EE

更新日期：2011-02-15 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：:Double-stranded RNA has become a ubiquitous tool for inhibition of gene expression in the laboratory. If similar success could be achieved in vivo, duplex RNA might provide a new class of therapeutics capable of treating a broad spectrum of disease. Chemists and biologists developing duplex RNA as a drug have made pro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Watts JK,Corey DR

更新日期：2010-06-01 00:00:00

abstract：:Two new technetium complexes containing a piperidine template have been synthesized and evaluated as possible leads for the development of dopamine transporter (DAT) imaging agents. Binding data for the corresponding rhenium complexes containing either a monoaminomonoamide (MAMA') or a diaminodithiol (DADT) chelating ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hoepping A,Babich J,Zubieta JA,Johnson KM,Machill S,Kozikowski AP

更新日期：1999-11-15 00:00:00

abstract：:A series of N-4-substituted-benzyl-N'-tert-butylbenzyl thioureas were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor in rat DRG neurons. Their structure-activity relationship reveals that not only the two oxygens and amide hydrogen of sulfonamido group, but also the optimal...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park HG,Choi JY,Choi SH,Park MK,Lee J,Suh YG,Cho H,Oh U,Lee J,Kang SU,Lee J,Kim HD,Park YH,Su Jeong Y,Kyu Choi J,Jew SS

更新日期：2004-02-09 00:00:00