Showing papers in "European Journal of Medicinal Chemistry in 2014"

TL;DR: This review article focuses on the recent developments (2010-2014) on various pharmacological and medicinal aspects of chalcones and their analogues.

TL;DR: The present review gives detail about the structural requirement of flavone derivatives for various pharmacological activities and may provide an opportunity to scientists of medicinal chemistry discipline to design selective, optimize as well as poly-functional flavones derivatives for the treatment of multi-factorial diseases.

TL;DR: This article is an effort to summarize recent developments in the environmentally benign synthetic methods providing access to quinazoline andQuinazolinone scaffolds with promising biological potential and discuss potential future directions on the development of more potent and specific analogues for various biological targets.

TL;DR: The present review focuses on the pharmacological profile of chromone derivatives in the current literature with an update of recent research findings on this nucleus and the perspectives that they hold for future research.

TL;DR: A detailed account of the design strategies employed for the synthesis of anticancer agents via molecular hybridization techniques is offered and the structure activity relationship along with mechanistic insights revealed during the biological evaluation of the hybrids are highlighted.

TL;DR: It is concluded that 6-brominated coumarin hydrazide-hydrazone derivatives 7c could be a potent anticancer drug to overcome drug resistance in cancer and it could be highly beneficial for patients in the clinic.

TL;DR: In the present review, published reports on benzimidazole scaffold are collated to provide an insight so that its full therapeutic potential can be utilized for the treatment of pain and inflammation.

TL;DR: This review highlights the various classes of synthetically derived chemical compounds those have been reported in last few years as potential tubulin polymerization inhibitors and a brief synthetic methodology to access these compounds has been highlighted along with the brief SAR studies.

TL;DR: The last section of the review encompasses the various patents granted on 4-thiazolidinone analogs/derivatives with World Intellectual Proprietary Organization and United State Patent Trademark Office (USPTO), particularly in the duration of the year 2000 to the year 2012.

TL;DR: Despite DNA being an important target for several drugs, most of the docking programs are validated only for proteins and their ligands, therefore, a default protocol to identify DNA binding modes which uses a modified canonical DNA as receptor is needed.

TL;DR: This review mainly focuses on the existence of isoxazoline derivatives in natural sources, their isolation and uses there of as anticancer agents besides highlighting the synthetic pathways to achieve these compounds.

TL;DR: The synthesis of silver nanoparticles using aqueous rhizome extract of Acorus calamus (ACRE) and evaluation of antioxidant, antibacterial as well as anticancer effects of synthesized A. calamusSilver nanoparticles (ACAgNPs) emphasize that such biocompatible green nanoparticles with multifaceted biological activities may find their applications in the field of nanomedicine.

TL;DR: Results verify that the attachment of an antibody on the curcumin-liposome surface does not block deposit staining or prevention of Aβ aggregation, while the presence of the cur cumin-PEG-lipid conjugate does not reduce their brain-targeting capability substantially, proving the potential of such multifunctional NLs for application in Alzheimer disease treatment and diagnosis.

TL;DR: The present review discusses various MFCs developed for specific class of disorders with an aim to provide an insight into the strategies in medicinal chemistry for development of such compounds.

TL;DR: Molecular docking suggested that the cytotoxicity of reported hybrids could be possibly due to their dual inhibition of α- and β-tubulins at GTP and colchicine binding sites, respectively, and falcipain-2 was identified to be a plausible target site of the hybrids given their antimalarial potency.

TL;DR: The anti-oxidant/anti-inflammatory and anticancer effects of kaempferol are summarized with a focus on its molecular targets and the possible use of this flavonoid for the treatment of inflammatory diseases and cancer.

TL;DR: A sincere attempt to compile the synthetic and design aspects of quinazoline derivatives with significant anticonvulsant action so that this structural class of compound can prove to be useful for the design and development of potent anticonVulsant agents.

TL;DR: This study has identified a new class of potent α-glucosidase inhibitors, based on the binding interactions of biscoumarin derivatives with the enzyme, that are applicable to the treatment of diabetes.

TL;DR: DPH6 was capable to significantly decrease scopolamine-induced learning deficits in healthy adult mice and was less toxic than donepezil at high concentrations; while at low concentrations both displayed a similar cell viability profile.

TL;DR: S1, the highest potency for both radical scavenging and AChE inhibitory activity, exhibited an ability to improve both short-term and long-term memory deficit in mice induced by scopolamine and can be considered as a candidate with potential impact for further pharmacological development in Alzheimer's therapy.

TL;DR: Compound 9a could effectively intercalate into Calf Thymus DNA to form 9a-DNA complex which might block DNA replication to exert their powerful antimicrobial activities, thus improving its antimicrobial efficacy.

TL;DR: It has been shown that both the positions of electronegative atoms like F and O in the pyrazole substituents and the amount of the associated charges on such atoms are crucial in regulating the strength of antifungal activity for the C. albicans strain.

TL;DR: A series of novel benzimidazole carbamates bearing indole moieties with sulphur or selenium atoms connecting the aromatic rings were synthesised and evaluated for their antiproliferative activities against three human cancer cell lines using an MTT assay.

TL;DR: The chal cone 38 containing an amino (-NH2) group on ring A was the most potent and selective against cancer cells and the effects of the chalcone 38 on regulation of 43 apoptosis-related markers in HT-29 cells were determined.

TL;DR: The potential use of these compounds as source of novel agents for the treatment of leishmaniasis is demonstrated and they exhibit strong antileishmanial activity that was even higher than that of Amphotericin B, with significant cytotoxicity.

TL;DR: These spirooxindole-pyrrolidine compounds can be promising therapeutic agents for A549 lung adenocarcinoma cancer cell line.

TL;DR: Current trends in the field of peptide-based pharmaceuticals are reviewed and naturally occurring cyclic disulfide-rich peptide scaffolds are described, discussing their pharmaceutically attractive properties and benefits.

TL;DR: The minimal inhibitory concentration of silver nanoparticles was recorded against most of the bacteria and fungus and MCF-7 human breast adenocarcinoma cancer cell line was employed to observe the efficacy of cancer cell killing.

TL;DR: It is found that, in general, and for the same substituent, amines are more potent ChE inhibitors or equipotent than the corresponding amides, showing a clear EeAChE inhibition selectivity.

TL;DR: The tested compounds proved to have better gastric safety profile compared to celecoxib, and the most potent and selective COX-2 inhibitors - compounds 3c, 3d, 3e, 9c and 9d - were assessed for their anti-inflammatory activity and ulcerogenic liability in vivo.