Showing papers in "European Journal of Medicinal Chemistry in 2013"

TL;DR: The present review is an attempt to understand the chemistry along with medicinal importance of pyrazole containing natural products reported till date which would certainly help the scientific community to bring further developments in the isolation and synthetic methodologies for pyrazoles based novel bioactive compounds.

TL;DR: A spectrum of strategies to design AChE inhibitors used in the Alzheimer therapy is given, which shows the most viable therapeutic target for the symptomatic treatment of AD.

TL;DR: The results revealed that the compound 11c having 2,5-dichlorothiophene substituent on pyrazole moiety and a triazole ring showed significant analgesic and antimicrobial activity.

TL;DR: This review summarizes the current progress in the basic, clinical, and translational research on natural products in treatment of various liver diseases and focuses on the discovery and biological evaluation of the natural products, which shows potential as a new therapeutic agent of liver diseases.

TL;DR: Flow cytometry analysis demonstrated that treatment of MGC-803 with 3c led to cell cycle arrest at G2/M phase accompanied by an increase in apoptotic cell death after 12 h, and compound 3a was more potent than 5-fluorouracil against all tested human cancer cell lines.

TL;DR: The results presented in this review may help to emphasize that these compounds could be promising as a new alternative for the treatment of cancer, either alone or in combination with other antitumor drugs to potentiate their effects.

TL;DR: The localization of carotenoids in biological membranes, their interactions and reactions with ascorbic acid and alpha-tocopherol as well as their redox potentials are discussed in view of their antioxidant properties as beneficial species in preventing various diseases.

TL;DR: Hydantoin derivative 6o with a 6-bromo-2-methyl-2H-chromene substructure showed the best profile of cytotoxicity comparable to that of cisplatin as standard anticancer agent.

TL;DR: The use of molecular modeling is reviewed in the designing of novel pyrazole analogs that may target various receptors such as protein kinase inhibitor, tyrosine kinases, Aurora-A kinase, tumor growth factor, cyclin dependent kinase (CDK) and fibroblast growth factor (FGF), which are significant for the management of cancer.

TL;DR: Kinetic and molecular modeling studies indicated that 8f was a mixed-type inhibitor, binding simultaneously to active, peripheral and mid-gorge sites of AChE, suggesting that8f might be an excellent multifunctional agent for AD treatment.

TL;DR: The structure of the newly compounds was confirmed on the basis of elemental analysis and spectral data and the inhibition of the carrageenin-induced oedema by these compounds was established.

TL;DR: The structure activity relationship revealed that the presence of electron withdrawing groups at para position of phenyl ring remarkably enhanced the antibacterial activity of synthesized compounds.

TL;DR: The thienotriazolopyrimidine derivatives 9, 13 and 14a were proved to display distinctive anti-inflammatory activity at the acute and subacute models as well as good analgesic profile with a delayed onset of action and are well tolerated by experimental animals with high safety margin.

TL;DR: SOD mimics with varying coligand are momentous in developing potential chemotherapeutic drugs and the pBR322 plasmid strand break offered by 2 + O₂·⁻ system reveals oxidative cleavage mechanism.

TL;DR: Bioassays conducted at Syngenta showed that several of the synthesized compounds exhibit higher antifungal activity than pimprinine, the natural product which inspired this synthesis.

TL;DR: The compound 5h (NCS: 760452, 1-(1H-benzo [d] imidazol-2-yl)-3-(6-dichlorophenyl)-[1,2,4]triazolo[3,4-b]thiadiazol-3-yl) propan-1-one) exhibited significant growth inhibition and may possibly be used as lead compound for developing new anticancer agents.

TL;DR: A new series of N-acetyl and N-formyl-pyrazoline derivatives 6 and 7-8 showed remarkable antitumor activity against cancer cell lines, with the most important GI50 values ranging from 0.13 to 0.99 μM.

TL;DR: Compound 8h, with an optimum alkyl chain length and a chloro substituent at the C-5 position of the isatin ring, displayed the best activity among the test compounds, with IC50 value of 1.21 μM against cultured W2-strain Plasmodium falciparum.

TL;DR: 5-acetyl-4-methyl-2-(3-pyridyl)thiazole (5) exhibited twofold antibacterial activity of ampicillin in inhibiting the growth of Staphylococcus epidermidis and also showed equipotent antifungal activity with amphotricin B against Geotricum candidum.

TL;DR: As evident from various biological end points, inhibition of cell migration and colony formation, mitochondrial membrane disruption followed by DNA fragmentation and apoptosis, is demonstrated.

TL;DR: The bioactive evaluation showed that 3,5-bis(trifluoromethyl)phenyl benzimidazoles gave comparable or even stronger antibacterial and antifungal efficiency in comparison with reference drugs Chloromycin, Norfloxacin and Fluconazole.

TL;DR: The docking study of the most potent compound 4m, indicated that Phe330 is responsible for ligand recognition and trafficking by forming π-cation interaction with benzylpiperidine moiety, which could stabilize the ligand in the active site resulting in more potent inhibition of the enzyme.

TL;DR: N-(4-(Pyrazol-4-yl)thiazol-2-yl)-N'-phenylthiourea derivative 2 was synthesized and then treated with variety of hydrazonoyl chlorides under basic condition at reflux to afford the corresponding 2-( 4-(pyrazol)-1,3,4-thiadiazole derivatives 6, 10a-e and 17a- e.

TL;DR: Structural-activity relationship (SAR) study using in-silico analysis matched well with in-vitro tumour cell inhibitory activity and all compounds exhibited very good phenyl hydrazine induced haemolysis of erythrocytes in phenylhydrazine assay.

TL;DR: A group of novel N-4-piperazinyl-ciprofloxacin-chalcone hybrids was prepared and one-dose anticancer test results indicated that compounds 3a and 3g exhibited the highest ability to inhibit the proliferation of different cancer cell lines.

TL;DR: A series of 2-(2-hydrazinyl)thiazole derivatives with a wide range of substitutions at 2-, 4- and 5-positions were designed by considering Lipinski rule to discover new potent inhibitors for Mycobacterium tuberculosis.

TL;DR: The kinetic study revealed that compound 10c exhibited mixed-type inhibition against AChE, and protein-ligand docking study demonstrated that the target compounds have dual binding site interaction mode, in agreement with kinetic study.

TL;DR: A series of novel 1,2,3-triazole-dithiocarbamate-urea hybrids were designed, synthesized and their antiproliferative activities against four selected human cancer cell lines were evaluated and showed that a number of the hybrids exhibited potent activity in selected humancancer cell lines.

TL;DR: New 5-aminopyrazoles 2a-c were prepared in high yields from the reaction of known α,α-dicyanoketene-N,S-acetal with hydrazine hydrate under reflux in ethanol, and the antibacterial activity and cytotoxicity against Vero cells of several selected compounds are reported.

TL;DR: The present review provides an overview about the progress in the discovery of Eg5 inhibitors especially from 2009 to 2012 as well as the clinical trials conducted on some of these inhibitors.