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Future Medicinal Chemistry

Longhuo Wu, Zhiping Liu
No abstract text is available yet for this article.
April 12, 2017: Future Medicinal Chemistry
Po Sing Leung
No abstract text is available yet for this article.
April 12, 2017: Future Medicinal Chemistry
Scott Harrison, Brian Lahue, Zhengwei Peng, Anthony Donofrio, Charlie Chang, Meir Glick
No abstract text is available yet for this article.
April 12, 2017: Future Medicinal Chemistry
Elismar Jn Cnossen, Amanda G Silva, Karina Marangoni, Rívia Ar Arruda, Evellyn G Souza, Fabiana Aa Santos, Patrícia T Fujimura, Jonny Yokosawa, Luiz R Goulart, Adriana F Neves
AIM: The dengue virus is responsible for a high worldwide incidence of infections, aggravated by late diagnosis, and often confused with other tropical diseases. Results/methodology: Oligonucleotide aptamers binding to the 5'-UTR from dengue virus selected after eight rounds by systematic evolution of ligands by exponential enrichment technology were analyzed by dot-blot assay and in silico prediction of secondary structures, demonstrating the presence of stem-loops that may have the potential for interaction with the viral genome, which can lead to loss of their original conformation...
April 12, 2017: Future Medicinal Chemistry
Hassanein H Hassanein, Hanan H Georgey, Marwa A Fouad, Ahmed M El Kerdawy, Mona F Said
AIM: The discovery of new generation of selective COX-2 inhibitors with potential analgesic and anti-inflammatory activity and minimal side effects is a major interest. MATERIALS & METHODS: Novel imidazole and imidazo[1,5-a]quinazoline derivatives were prepared and evaluated for their analgesic and anti-inflammatory activities. COX-1/COX-2 isozyme selectivity testing and molecular docking were performed. Key physicochemical parameters were calculated. RESULTS: All tested compounds exhibited significant activities compared with indomethacin as reference drug...
April 10, 2017: Future Medicinal Chemistry
Laiba Arshad, Md Areeful Haque, Syed Nasir Abbas Bukhari, Ibrahim Jantan
Curcumin, extracted mainly from Curcuma longa rhizomes, has been reported to possess potent anti-inflammatory and anti-oxidant activities. Although safe at higher doses and exhibiting multiple biological activities, curcumin still has the problem of poor bioavailability which has been an attractive area of research over the last few years. A number of efforts have been made by modifying structural features of curcumin. This review highlights the structurally modified and more stable newly synthesized curcumin analogs that have been screened against antioxidant and anti-inflammatory activities...
April 10, 2017: Future Medicinal Chemistry
Sotirios Katsamakas, Theodora Chatzisideri, Savvas Thysiadis, Vasiliki Sarli
Conjugates of cytotoxic agents with RGD peptides (Arg-Gly-Asp) addressed to ανβ3, α5β1 and ανβ6 integrin receptors overexpressed by cancer cells, have recently gained attention as potential selective anticancer chemotherapeutics. In this review, the design and the development of RGD conjugates coupled to different small molecules including known cytotoxic drugs and natural products will be discussed.
April 10, 2017: Future Medicinal Chemistry
(no author information available yet)
No abstract text is available yet for this article.
March 23, 2017: Future Medicinal Chemistry
Thet Su Win, Aijaz Ahmad Malik, Virapong Prachayasittikul, Jarl E S Wikberg, Chanin Nantasenamat, Watshara Shoombuatong
AIM: Toxicity arising from hemolytic activity of peptides hinders its further progress as drug candidates. MATERIALS & METHODS: This study describes a sequence-based predictor based on a random forest classifier using amino acid composition, dipeptide composition and physicochemical descriptors (named HemoPred). RESULTS: This approach could outperform previously reported method and typical classification methods (e.g., support vector machine and decision tree) verified by fivefold cross-validation and external validation with accuracy and Matthews correlation coefficient in excess of 95% and 0...
February 17, 2017: Future Medicinal Chemistry
Makrina Totsika
No abstract text is available yet for this article.
February 16, 2017: Future Medicinal Chemistry
Pawin Pongkorpsakol, Aekkacha Moonwiriyakit, Chatchai Muanprasat
Nutrient-sensing receptors, including fatty acid receptors (FFA1-FFA4), Ca(2+)-sensing receptors and Zn(2+)-sensing receptors, are involved in several biological processes. These receptors are abundantly expressed in the GI tract, where they have been shown to play crucial roles in regulating GI function. This review provides an overview of the GI functions of fatty acid and mineral receptors, including the regulation of gastric and enteroendocrine functions, GI motility, ion transport and cell growth. Recently, several lines of evidence have implicated these receptors as promising therapeutic targets for the treatment of GI disorders, for example, inflammatory bowel disease, colorectal cancer, metabolic syndrome and diarrheal diseases...
February 16, 2017: Future Medicinal Chemistry
Lixia Gao, Catherine E Jauregui, Yong Teng
Autophagy is a self-protective mechanism of living cells or organisms under various stress conditions. Studies of human genetics and pathophysiology have implicated that alterations in autophagy affect the context of cellular homeostasis and disease-associated phenotypes. The molecular components of autophagy are currently being explored as new pharmacologic targets for drug development and therapeutic intervention of various diseases. Drugs that restore the normal autophagic pathways have the potential for effectively treating human disorders that depend on aberrations of autophagy...
February 8, 2017: Future Medicinal Chemistry
Fátima Morales, Alberto Ramírez, Cynthia Morata-Tarifa, Saúl A Navarro, Juan A Marchal, Joaquín M Campos, Ana Conejo-García
AIM: Cancer is among the leading causes of death worldwide. Medical interest has focused on macrocyclic polyamines because of their properties as antitumor agents. Results/Methodology: We have designed and synthesized a series of 1,2-diaminocyclohexane derivatives with notable in vitro antiproliferative activities against the MCF-7, HCT-116 and A375 cancer cell lines. Cell cycle and apoptosis analyses were also carried out. Our results show that all the compounds are potent cytotoxic agents, especially against the A375 cell line...
February 8, 2017: Future Medicinal Chemistry
Bernard T Golding
No abstract text is available yet for this article.
February 8, 2017: Future Medicinal Chemistry
Hendra Gunosewoyo, Lifang Yu, Lenka Munoz, Michael Kassiou
Originally thought to be nondruggable, kinases represent attractive drug targets for pharmaceutical companies and academia. To date, there are over 40 kinase inhibitors approved by the US FDA, with 32 of these being small molecules, in addition to the three mammalian target of rapamycin inhibitor macrolides (sirolimus, temsirolimus and everolimus). Despite the rapid development of kinase inhibitors for cancer, presently none of these agents are approved for CNS indications. This mini perspective highlights selected kinase targets for CNS disorders, of which brain-permeable small-molecule inhibitors are reported, with demonstrated preclinical proof-of-concept efficacy...
February 8, 2017: Future Medicinal Chemistry
Giuseppe Deganutti, Stefano Moro
Kinetic and thermodynamic ligand-protein binding parameters are gaining growing importance as key information to consider in drug discovery. The determination of the molecular structures, using particularly x-ray and NMR techniques, is crucial for understanding how a ligand recognizes its target in the final binding complex. However, for a better understanding of the recognition processes, experimental studies of ligand-protein interactions are needed. Even though several techniques can be used to investigate both thermodynamic and kinetic profiles for a ligand-protein complex, these procedures are very often laborious, time consuming and expensive...
April 2017: Future Medicinal Chemistry
Kenneth Lundstrom
No abstract text is available yet for this article.
April 2017: Future Medicinal Chemistry
Shinya Fujii, Yuichi Hashimoto
Application of silyl functionalities is one of the most promising strategies among various 'elements chemistry' approaches for the development of novel and distinctive drug candidates. Replacement of one or more carbon atoms of various biologically active compounds with silicon (so-called sila-substitution) has been intensively studied for decades, and is often effective for alteration of activity profile and improvement of metabolic profile. In addition to simple C/Si exchange, several novel approaches for utilizing silicon in medicinal chemistry have been suggested in recent years, focusing on the intrinsic differences between silicon and carbon...
April 2017: Future Medicinal Chemistry
Mostafa Mm El-Miligy, Aly A Hazzaa, Hanan El-Messmary, Rasha A Nassra, Soad Am El-Hawash
AIM: Simultaneous inhibition of 5-LOX/COX may enhance anti-inflammatory effects and reduce side effects. Hence, synthesis of novel dual inhibitors of 5-LOX/COX is an important strategy for treatment of inflammation. Results/methodology: The target compounds were designed to hybridize benzothiophene scaffold or its bioisostere benzofuran with various anti-inflammatory pharmacophore hetercycles through different atoms spacers. Compounds 4a, 4c, 4d, 5b, 7a, showed significant in vitro LOX inhibitory activity higher than that of meclofenamate sodium...
April 2017: Future Medicinal Chemistry
Pankaj Kumar Singh, Om Silakari
AIM: Different resistance mechanisms, especially, T790M secondary acquired point mutation and in some cases amplification of cMET, have been a major setback for the lung cancer therapies. METHODOLOGY: The current in silico study explored the small molecules which can act as putative EGFR (T790M)-cMET dual inhibitors. Databases were first filtered and subsequently cross filtered, initially by thoroughly validated pharmacophore models for both targets. As per score and interactions obtained in docking, the molecules were subjected to molecular dynamics simulations, to study the stability and binding orientations of their complexes with target proteins...
April 2017: Future Medicinal Chemistry
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