Showing papers in "European Journal of Medicinal Chemistry in 2015"

TL;DR: This Review Article is focused on the action of the reactive oxygenated species in inducing oxidative injury of the lipid membrane components, as well as on the ability of antioxidants (of different structures and sources, and following different mechanisms of action) in fighting against oxidative stress.

TL;DR: This review highlights recent progress of biologically active spirooxindoles for their anticancer potentials, mainly focusing on the discussions of SARs and modes of action.

TL;DR: This review focused on the recent development of indole derivatives as antiviral agents and summarized the structure property, hoping to inspire new and even more creative approaches to discover novel drugs with different modes of action.

TL;DR: This review has compiled and discussed specifically the anticancer potential of quinoline derivatives, which could provide a low-height flying bird's eye view of theQuinoline derived compounds to a medicinal chemist for a comprehensive and target oriented information for development of clinically viable anticancer drugs.

TL;DR: A comprehensive study on molecular targets/pathways involved in carcinogenesis, mechanism of actions (MOAs), structure activity relationships (SARs) and patents granted have been highlighted and may be helpful for (medicinal) chemists to design more potent, safe, selective and cost effective anti-cancer chalcones.

TL;DR: The present review is endeavour to highlight the progress in the various pharmacological activities of benzofuran derivatives in the current literature with an update of recent research findings on this nucleus.

TL;DR: This is the first standalone review that emphasis on the assorted retrosynthetic approaches, important targets for molecularly targeted cancer therapy and structure activity relationship studies that highlight the chemical groups responsible for evoking the anticancer potential of coumarin derivatives reported from 2011 to 2014.

TL;DR: The current developments of coumarin-based anticancer agents are covered and the structure-activity relationship of the most potent compounds are discussed.

TL;DR: This work systematically gives a comprehensive review in current developments of BTA-based compounds in the whole range of medicinal chemistry as anticancer, antibacterial, antifungal, antiinflammatory, analgesic, anti-HIV, antioxidant, anticonvulsant, antitubercular, antidiabetic, antileishmanial, antihistaminic, antimalarial and other medicinal agents.

TL;DR: The structures of 1H-pyrazoles with their corresponding biological activities for 21st (in 2000-2014 years) century are reported.

TL;DR: Recent developments in the eco-friendly and green procedures for the construction of highly challenging and potentially bioactive quinazoline and quinzolinone compounds are recapitulate in order to help medicinal chemists in designing and synthesizing novel and potent compounds for the treatment of different disorders.

TL;DR: In this review the State of the Art will be presented, which includes a summary of the progress made over the past years in the knowledge of the structure and mechanism of the quinoxaline and quInoxaline derivatives, associated medical and biomedical value as well as industrial value.

TL;DR: The present manuscript to the best of the authors' knowledge is the first compilation on synthesis and medicinal aspects including structure-activity relationships of benzimidazole reported to date.

TL;DR: The strategy involved investigation on understanding the chemistry behind the antioxidant activities of BHT, whether through hydrogen or electron transfer mechanism to enable promising anti-oxidant candidates to be synthesized.

TL;DR: The most important biological effects of thiazole-based compounds are reviewed and their roles in new leads identification and drug discovery are highlighted to help researches for finding potential future directions on the development of more potent and specific analogs of th Diazole- based compounds for various biological targets.

TL;DR: Technological advancements and emerging chemical approaches for stabilizing active peptide conformations, including stapling, hydrogen bond surrogates, beta-hairpin mimetics, grafting on stable scaffolds, and macrocyclization are described, carrying the promise of opening the doors for peptide therapeutics to reach the currently "undruggable" space.

TL;DR: The literature reports of thiazoles and benzothiazoles possessing different biological activities are disclosed and it is disclosed that the thiazole moiety is abundantly found in natural products while BenzothiazoleMoiety is rare.

TL;DR: This review focuses on novel routes of their synthesis and various biological activities of fused aromatic 1H and 2H-indazoles.

TL;DR: The review gives in the end a brief overview of the potential of Mannich bases as inhibitors of various enzymes or ligands for several receptors.

TL;DR: This article emphasizes on the importance of benzofuran as a biologically relevant heterocycle and covers most of the physiologically as well as medicinally important compounds containing benz ofuran rings.

TL;DR: The present review focuses on the recent progress in knowledge on various biological properties of classical, tricyclic carbazole derivatives from 2010 until now.

TL;DR: The compounds which showed promising activity and have a well-defined MOAs, SARs must be considered as prototype for the design and development of potential anti-diabetic agents to meet the demand of diabetics.

TL;DR: The present review will provide an insight on lead design-developments of the decade, clinical candidates and PET tracer radio-ligands containing benzofuran core along with brief target biology.

TL;DR: This mini-review attempts to highlight the importance of moracins, as they have been a major source for drug development, and summarizes the current state of the art concerning the synthesis and medicinal use ofmoracins A-Z.

TL;DR: This review collated published reports on coumarin derivatives to shed light on the insights on different types of methods reported for their preparations, characterizations and anti-TB applications, so that its full therapeutic potential class of compounds can be utilized for the treatment of tuberculosis.

TL;DR: A review finds those "needles" in that haystack and lays groundwork for highlighting promising α-glucosidase inhibitors from the literature that may potentially become suitable candidates for pre-clinical or clinical trials while drawing attention of the drug development community to consider and take already-identified promisingα-glUCosid enzyme inhibitors into the next stage of drug development.

TL;DR: Examples of in silico discoveries of tyrosine kinase inhibitors and bromodomain antagonists whose binding mode was predicted by automated docking and further corroborated by MD simulations with final validation by X-ray crystallography are presented.

TL;DR: This review contains various pharmacological activities of 1,2,4-triazole-3-thiones in one place and it is also the milestone for the new research towards this moiety.

TL;DR: The predicted physico-chemical properties indicated the drug appropriateness for most of these compounds, as they obey Lipinski's rule of five (RO5), and a new class of α-glucosidase inhibitors was identified.

TL;DR: A series of forty different pyrazole containing benzimidazole hybrids have been designed, synthesized and evaluated for their potential anti-proliferative activity against three human tumor cell lines - lung, breast, and cervical.