Showing papers in "Bioorganic & Medicinal Chemistry Letters in 2010"

TL;DR: In this Letter, the structure-activity relationships, optimization of design, testing criteria, and human half-life data for a series of selective COX-2 inhibitors are provided.

TL;DR: The most promising compound 26 showed around 30-fold more selectivity towards C33A (cervical carcinoma) cells over normal fibroblast NIH3T3 cells with an IC(50) value of 3.59 μM.

TL;DR: A series of N-(2-amino-5-substituted phenyl)benzamides were designed, synthesized and evaluated for their inhibition of HDAC2 and their cytotoxicity in HCT116 cancer cells.

TL;DR: Some N-substituted carbazole derivatives displayed comparable or even better antibacterial and antifungal activities than reference drugs fluconazole, chloramphenicol and norfloxacin against tested strains.

TL;DR: Indolyl chalcones 3l and 3m were identified as the most potent and selective anticancer agents with IC(50) values 0.03 and 0.09 microM, against PaCa-2 cell line, respectively.

TL;DR: A novel pentacyclic indolosesquiterpene, named xiamycin, and its methyl ester have been obtained from Streptomyces sp.

TL;DR: The analysis of the widely consumed synthetic N-methyl-cathinone analogue known as mephedrone and its spectral data and molecular properties indicated that the methyl- cathinones are considerably more hydrophilic than themethyl-amphetamines which may account for the higher doses that are needed to demonstrate similar effects.

TL;DR: Two series of disubstituted coumarins incorporating ether and acetyl/propionyl moieties in positions 6,7- and 7,8- of the heterocyclic ring were synthesized investigated for the inhibition of the zinc enzyme carbonic anhydrase.

TL;DR: Three new aminolipopeptides, designated trichoderins A, A1 (2), and B (3), were isolated from a culture of marine sponge-derived fungus of Trichoderma sp.

TL;DR: A series of polyphenolic derivatives, including resveratrol, dobutamine, curcumin, catechin and silymarine were investigated for the inhibition of all the catalytically active mammalian isozymes of the metalloprotein carbonic anhydrase, showing quite diverse inhibition profiles with these compounds.

TL;DR: The ability of the compounds to inhibit soybean lipoxygenase was determined as an indication of potential anti-inflammatory activity and the in vitro antioxidant activity of the synthesized compounds was evaluated.

TL;DR: The antimalarial data for this series suggests that growth inhibition of the W2 strain of Plasmodium falciparum can be imparted by the introduction of a methoxy group ortho to the acetylenic group.

TL;DR: All quinone-methide triterpenes 1–4 have proven to be competitive by the kinetic analysis and show potent inhibitory activities in A-ring and more hydrophobic E-ring assist to exhibit potent activity.

TL;DR: Gold nanoparticles coated with multiple copies of an amphiphilic sulfate-ended ligand are able to bind the HIV envelope glycoprotein gp120 as measured by surface plasmon resonance (SPR) and inhibit in vitro the HIV infection of T-cells at nanomolar concentrations.

TL;DR: These agents represent the second reported chemotype for activation of PKM2 based upon a substituted thieno-pyrrole-based scaffold and are described as a potential strategy for returning cancer cells to a metabolic state characteristic of normal cells.

TL;DR: 6-Hydroxycoumarin showed K(I)s >100 microM against CA I and II, being thus a selective, efficient inhibitor for the tumor-associated over cytosolic isoforms, and excellent leads for designing isoform-selective enzyme inhibitors.

TL;DR: Series of pyrolidine analogues were synthesized and examined as acetylcholinesterase (AChE) inhibitors, and compounds 4k and 6k were the most potent inhibitors of the series.

TL;DR: Key studies leading to the discovery and definition of the role of endogenous fatty acid amide signaling molecules are summarized.

TL;DR: The ionic liquids with alkyl substitution of C-12 chain length were found to be effective against all 60 tumor cell lines and show very low cytotoxicity in most of the cases.

TL;DR: A series of pyrimidine nucleoside-pyrano[3,2-c]pyridone or pyrano(4,3-b)pyran hybrids were efficiently obtained and showed encouraging biological activities.

TL;DR: In vitro antitubercular screening of 27 compounds against Mycobacterium tuberculosis H37Rv disclosed that spiro[5.3']-5'-nitrooxindolespiro has the maximum potency with a minimum inhibitory concentration (MIC) of 1.4 μM against MTB, being 3.4 and 5.4 times more potent than ciprofloxacin and ethambutol, respectively.

TL;DR: Compound 4 was more active against brine shrimp than the others, and 3 possessed potent activity against Escherichia coli.

TL;DR: A simple and highly efficient method has been developed for the synthesis of 3,3-diindolyl oxyindoles by the reaction of indoles with isatin or 5-fluoro isatin using a catalytic amount of FeCl(3) at room temperature in a short reaction time in high yields.

TL;DR: The results of the studies reveal that the chalcones with N-methyl piperazine methyl and piperidine methyl substitution seems to be important for inhibition of beta-glucuronidase.

TL;DR: 4-Methoxyphenyl substituted 1,3-oxazoheterocycle fused 1,2, 3-triazole 6j was found to be the most potent derivative with IC(50) values lower than 1.9 microg/mL against A431 and K562 human tumour cell lines.

TL;DR: Structural-activity relationship analysis demonstrates that o-dihydroxyl groups on the aromatic A ring and 4-hydroxyl group attached to the aromatic B ring contribute critically to the antioxidant and antiproliferative activities.

TL;DR: A novel double pro-drug approach applied to the anti-HCV agent 2'-beta-C-methyl guanosine leads to a compound INX-08189 that exhibits 10nM potency in the HCV genotype 1b subgenomic replicon, thus being 500 times more potent than the parent nucleoside.

TL;DR: A simple and efficient method for the one-pot three-component synthesis of new spirooxindoles in room temperature is described and the results are good on comparison with of standard antibacterial compounds.

TL;DR: N-substituted-3-carboxamido-coumarin derivatives were prepared and evaluated for selective antibacterial activity against 20 isolates of Helicobacter pylori clinical strains, including five metronidazole resistant ones.

TL;DR: A series of novel coumarin bisindole heterocycles synthesized following an uncommon method showed potent antihyperlipidemic activity and was found to decrease the plasma triglyceride levels, total cholesterol, and HDL-C/TC ratio in hyper Lipidemic rats to a greater degree than some of the reference statins.