Showing papers in "European Journal of Medicinal Chemistry in 2018"

TL;DR: The possible side effects that MTX might cause from the most common gastrointestinal toxicity effects to less frequent malignant diseases are reviewed to provide scholars with a comprehensive understanding of the side effects of MTX administration by RA patients.

TL;DR: The role of quercetin and its derivatives may go beyond their existence in food and has potential as a lead molecule in drug development programs as well as mechanisms to observe cardiovascular diseases such as aging effects, hypertension, angiotensin-converting enzyme activity and endothelial-dependent and independent functions.

TL;DR: Natural preservatives could also constitute a viable alternative to address the critical problem of microbial resistance, and to hamper the negative side effects of some synthetic compounds, while meeting the requirements for food safety, and exerting no negative impact on nutritional and sensory attributes of foodstuffs.

TL;DR: This review summarizes the findings about natural compounds as chemoprotective agents for decreasing risk of CRC and identifies natural compounds which possess anti-tumor effects of various characteristics.

TL;DR: The present article aims to review the current application of indole core in the design of new anticancer agents that may act via various targets such as histone deacetylases, sirtuins, PIM kinases, DNA topoisomerases and σ receptors.

TL;DR: This work systematically reviewed the recent researches and developments of the whole range of oxazole compounds as medicinal drugs, including antibacterial, antifungal, antiviral, antitubercular, anticancer, anti-inflammatory and analgesic, antidiabetic, antiparasitic, anti -obesitic,Anti-neuropathic, antioxidative as well as other biological activities.

TL;DR: This review offers a medium on which future drug design and development toward diabetes management may be modelled (i.e. optimization via structural derivatization), as many of the drug candidates highlighted show promise as an effective anti-diabetic chemotherapy.

TL;DR: The recent advances made towards the discovery of ciprofloxacin derivatives as antibacterial agents and the structure-activity relationship of these derivatives was also discussed.

TL;DR: An overview of recent literature is presented to provide imminent into the applications of different heterocyclic scaffolds in fighting against malaria.

TL;DR: Keap1, a substrate adaptor protein for ubiquitin E3 ligase involved in oxidative stress regulation, is identified as a novel candidate for PROTACs that can be applied in the degradation of the nonenzymatic protein Tau and peptide 1 can downregulate the intracellular Tau level in both time- and concentration-dependent manner.

TL;DR: A comprehensive review of the medicinal chemistry aspects in the development of various classes of nitrogen mustards (mechlorethamine, chlorambucil, melphalan, cyclophosphamide and steroidal based nitrogenmustards) including the historical and the latest developments in these areas are discussed.

TL;DR: This study developed MS4748 and MS4740, very close analogs of 5 and 6 respectively, which are incapable to degrade the ALK fusion proteins, as negative controls, which paved the way for developing the next generation of ALK PROTACs.

TL;DR: Terpenes' medicinal properties are supported by numerous in vitro, animal and clinical trials and show anti-inflammatory, antioxidant, analgesic, anticonvulsive, antidepressant, anxiolytic, anticancer, antitumor, neuroprotective, anti-mutagenic,Anti-allergic, antibiotic and anti-diabetic attributes, among others.

TL;DR: This review article comprises the tamoxifen derivatives reported in the literature in the last few years and it is anticipated that it will assist medicinal chemists in the synthesis of novel and pharmacologically potent agents for various therapeutic targets.

TL;DR: Current review focus on the discoveries of dual targeting agents in cancer therapy using rational, computational, proteomic, bioinformatics and polypharmacological approach that enables the discovery and rational design of effective and safe multi-target anticancer agents.

TL;DR: This review focuses on the TMP analogs that are designed based on CA-4, indole, chalcone, colchicine and natural product scaffolds which are known to interact with the colchichine binding site in tubulin.

TL;DR: This review principally emphases on the medicinal chemistry aspects including drug design, structure-activity relationships (SARs), and mechanism of actions of quinazoline derivatives.

TL;DR: The synthesized quinoline derivatives bearing pyrazole moiety are interesting scaffolds for the development of novel antibacterial and antifungal agents according to the tested strains of bacteria and fungi.

TL;DR: The enriched SAR paves the way to the further rational development of 4-quinolones with a unique mechanism of action different from that of the currently used drugs to overcome the resistance, well-tolerated and low toxic profiles.

TL;DR: This review focusses on recent advancements; pertaining to pyrrole scaffold, discussing various aspects of structure activity relationship and its bioactivities.

TL;DR: This review presents the current state of the art of DHPM biological activities and demonstrates that there is still a need for further in vivo studies to better delineate the pharmacological potential of this class of substances.

TL;DR: The synthesis of 22 new substances belonging to two classes of compounds, thiosemicarbazones and thiazoles, with the purpose of developing new drugs that present high specificity for tumor cells and low toxicity to the organism are reported.

TL;DR: The present review surveys the pharmacological advantages and deficiencies of both reversible and irreversible BTK drugs, with a focus on the structure-activity relationship (SARs) and binding modes of representative drugs, which could inspire critical thinking and new ideas for developing potent BTK inhibitors with less unwanted off-target effects.

TL;DR: This review focuses on the natural sources, structural features, mechanisms of action, structure-activity relationship (SAR) and chemical synthesis of MSAs, which mainly include paclitaxel, taccalonolides, epothilones, and FR182877 (cyclostreptin).

TL;DR: Concerns and opinions about development of donepezil derivatives, designing of MTDLs, and perspectives for AD treatments are discussed in final part.

TL;DR: Increasing evidences highlight the central role of ACLY, conferring a great therapeutic potential to this enzyme as a key target for the treatment of cancer, as well as the main ACLY inhibitors reported in the literature.

TL;DR: A comprehensive review of the literature on xanthones as inhibitors of α-glucosidase activity, their mechanism of action, experimental procedures and structure-activity relationships have been reviewed for more than 280 analogs.

TL;DR: The structural optimization analysis of coumarin suggest that derivatives 9, 13, 14, 18 and 19 could be a viable way of preventing and controlling bacteria and considered as promising lead compounds for the development of commercial drugs.

TL;DR: The aim of this review is to report those natural and synthetic compounds displaying significant antioxidant and antibacterial activities, and to select some selected synthetic compounds with an in-built capacity to act on two targets or with the combination in a single structure of two pharmacophores with antioxidant and antimicrobial activities.

TL;DR: The attributes of BODIPY derivatives for applications as antimicrobial photosensitizing agents can selectively bind to microbial cells, inducing an effective photokilling of pathogenic microbial cells.