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Future Medicinal Chemistry

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https://www.readbyqxmd.com/read/28795599/antimicrobial-2-aminothiazolyl-quinolones-what-is-their-potential-in-the-clinic
#1
Wei-Wei Gao, Cheng-He Zhou
No abstract text is available yet for this article.
August 10, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28795598/inhibition-studies-of-dna-methyltransferases-by-maleimide-derivatives-of-rg108-as-non-nucleoside-inhibitors
#2
Grégoire Rondelet, Laurence Fleury, Céline Faux, Véronique Masson, Jean Dubois, Paola B Arimondo, Luc Willems, Johan Wouters
AIM: DNA methyltransferases (DNMTs) are important drug targets for epigenetic therapy of cancer. Nowadays, non-nucleoside DNMT inhibitors are in development to address high toxicity of nucleoside analogs. However, these compounds still have low activity in cancer cells and mode of action of these compounds remains unclear. MATERIALS & METHODS: In this work, we studied maleimide derivatives of RG108 by biochemical, structural and computational approaches to highlight their inhibition mechanism on DNMTs...
August 10, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28795595/what-is-the-future-for-fragment-based-drug-discovery
#3
György M Keserű, Michael M Hann
No abstract text is available yet for this article.
August 10, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28795593/small-molecule-inhibitors-for-acute-myeloid-leukemia-where-is-the-field-heading
#4
Paul C Trippier
No abstract text is available yet for this article.
August 10, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28795592/semi-synthetic-thymoquinone-analogs-new-prototypes-as-potential-antihyperlipidemics-in-irradiated-rats
#5
Nashwa H Zaher, Engy R Rashed, Mona A El-Ghazaly
AIM: Thymoquinone (TQ), has been reported to possess strong antihyperlipidemic properties. However, a variety of serious side effects has been reported for TQ. The present study aimed to evaluate the potential antihyperlipidemic activity of newly synthesized TQ analogs. METHODS & RESULTS: first, novel TQ derivatives were studied against radiation-induced dyslipidemia in male rats. Second, the most promising sulfur derivatives (4-7), were further tested to elucidate their possible mechanism(s) of actions...
August 10, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28795589/a-novel-series-of-n-pyridin-2-yl-4-thiazol-5-yl-pyrimidin-2-amines-as-highly-potent-cdk4-6-inhibitors
#6
Solomon Tadesse, Ge Zhu, Laychiluh B Mekonnen, Jimma L Lenjisa, Mingfeng Yu, Michael P Brown, Shudong Wang
AIM: Inhibitors of CDK4/6 have emerged as a powerful class of therapeutics for treatment of several malignancies. We herein describe the identification of a new series of molecules that demonstrated excellent selectivity for CDK4/6 over CDKs1, 7 and 9. RESULTS: Medicinal chemistry optimization led to the discovery of 58 and 69 that inhibited CDK4 and CDK4/6, respectively, with high potency and selectivity, and 58 and 69 exhibited potent antiproliferative activities in a panel of human cancer cell lines including leukemia, and cancers of the breast, colon, ovary, pancreas and prostate...
August 10, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28793800/anti-inflammatory-and-antioxidative-effects-of-camellia-oleifera-abel-components
#7
Xiaomei Xiao, Liangmei He, Yayun Chen, Longhuo Wu, Lin Wang, Zhiping Liu
Camellia oleifera Abel is a member of Camellia, and its seeds are used to extract Camellia oil, which is generally used as cooking oil in the south of China. Camellia oil consists of unsaturated fatty acids, tea polyphenol, squalene, saponin, carrot element and vitamins, etc. The seed remains after oil extraction of C. oleifera Abel are by-products of oil production, named as Camellia oil cake. Its extracts contain bioactive compounds including sasanquasaponin, flavonoid and tannin. Major components from Camellia oil and its cake have been shown to have anti-inflammatory, antioxidative, antimicrobial and antitumor activities...
August 10, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28792235/antimicrobial-efficacy-of-irradiation-with-visible-light-on-oral-bacteria-in-vitro-a-systematic-review
#8
Andreas Pummer, Helge Knüttel, Karl-Anton Hiller, Wolfgang Buchalla, Fabian Cieplik, Tim Maisch
AIM: Resistances to antibiotics employed for treatment of infectious diseases have increased to alarming numbers making it more and more difficult to treat diseases caused by microorganisms resistant to common antibiotics. Consequently, novel methods for successful inactivation of pathogens are required. In this instance, one alternative could be application of light for treatment of topical infections. Antimicrobial properties of UV light are well documented, but due to its DNA-damaging properties use for medical purposes is limited...
August 9, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28791911/targeting-species-specific-trace-amine-associated-receptor-1-ligands-to-date-perspective-of-the-rational-drug-design-process
#9
Elena Cichero, Michele Tonelli
G-protein-coupled receptors represent main targets of several clinically relevant drugs, playing nowadays a leading part for further drug discovery process. Trace amine-associated receptor's family (TAARs) assumed an intriguing role as druggable target in medicinal chemistry, being TAAR1 the most investigated. Indeed, related ligands proved to be intertwined in several circuits involved in pathological pathways or therapeutic routes. Herein, we highlight relevant efforts in the search of novel agonists, focusing on responsiveness featured by different chemotypes toward rodent and human TAAR1, in order to explore species-specificity preferences...
August 9, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28791894/decoding-hiv-resistance-from-genotype-to-therapy
#10
Irene T Weber, Robert W Harrison
Genetic variation in HIV poses a major challenge for prevention and treatment of the AIDS pandemic. Resistance occurs by mutations in the target proteins that lower affinity for the drug or alter the protein dynamics, thereby enabling viral replication in the presence of the drug. Due to the prevalence of drug-resistant strains, monitoring the genotype of the infecting virus is recommended. Computational approaches for predicting resistance from genotype data and guiding therapy are discussed. Many prediction methods rely on rules derived from known resistance-associated mutations, however, statistical or machine learning can improve the classification accuracy and assess unknown mutations...
August 9, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28789563/molecular-modeling-enzyme-activity-anti-inflammatory-and-antiarthritic-activities-of-newly-synthesized-quinazoline-derivatives
#11
Hatem A Abuelizz, Anouar El Hassane, Mohamed Marzouk, Essam Ezzeldin, Azza A Ali, Rashad Al-Salahi
AIM: 16 thioxoquinazolines were evaluated in vivo for anti-inflammatory activity using carrageenan-induced paw edema assay. RESULTS: In particular, out of the targets (1-16), compounds 4 and 6 displayed the highest anti-inflammatory activity (≥80%) and furtherly tested against complete Freund's adjuvant-induced arthritic rats. Significant reduction in the serum level of IL-1β, COX-2 and prostaglandin E2 in the complete Freund's adjuvant rats is demonstrated by compounds 4 and 6...
August 9, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28776416/synthetic-agonists-of-nod-like-rig-i-like-and-c-type-lectin-receptors-for-probing-the-inflammatory-immune-response
#12
Amy E Nielsen, Joseph D Hantho, Rock J Mancini
Synthetic agonists of innate immune cells are of interest to immunologists due to their synthesis from well-defined materials, optimized activity, and monodisperse chemical purity. These molecules are used in both prophylactic and therapeutic contexts from vaccines to cancer immunotherapies. In this review we highlight synthetic agonists that activate innate immune cells through three classes of pattern recognition receptors: NOD-like receptors, RIG-I-like receptors, and C-type lectin receptors. We classify these agonists by the receptor they activate and present them from a chemical perspective, focusing on structural components that define agonist activity...
August 4, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28771047/design-and-synthesis-of-some-new-2-3-bipyridine-5-carbonitriles-as-potential-anti-inflammatory-antimicrobial-agents
#13
Perihan A Elzahhar, Salwa Elkazaz, Raafat Soliman, Alaa A El-Tombary, Hossam A Shaltout, Ibrahim M El-Ashmawy, Abeer E Abdel Wahab, Soad A El-Hawash
AIM: Inflammation may cause accumulation of fluid in the injured area, which may promote bacterial growth. Other reports disclosed that non-steroidal anti-inflammatory drugs may enhance progression of bacterial infection. RESULTS: This work describes synthesis of new series of 2,3'-bipyridine-5-carbonitriles as structural analogs of etoricoxib, linked at position-6 to variously substituted thio or oxo moieties. Biological screening results revealed that compounds 2b, 4b, 7e and 8 showed significant acute and chronic AI activities and broad spectrum of antimicrobial activity...
August 3, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28771039/harnessing-the-regulators-to-enhance-viral-vaccine-efficacy
#14
Jagadeesh Bayry
No abstract text is available yet for this article.
August 3, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28771037/immunotherapy%C3%A2-a-pursuit-race-to-tomorrow-s-medicines
#15
Antonio Macchiarulo
No abstract text is available yet for this article.
August 3, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28771036/small-molecule-antagonists-of-the-immune-checkpoint-pathways-concept-to-clinic
#16
Pottayil G Sasikumar, Murali Ramachandra
No abstract text is available yet for this article.
August 3, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28771035/downregulation-of-p-selectin-glycoprotein-ligand-1-as-a-potential-anti-inflammatory-mechanism
#17
Gerd K Wagner
No abstract text is available yet for this article.
August 3, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28771034/in-silico-discovery-and-therapeutic-potential-of-ido1-and-tdo2-inhibitors
#18
Finith E Jernigan, Lijun Sun
No abstract text is available yet for this article.
August 3, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28771031/challenges-in-the-design-of-reliable-immuno-oncology-mouse-models-to-inform-drug-development
#19
Giada Mondanelli, Claudia Volpi, Ciriana Orabona, Ursula Grohmann
No abstract text is available yet for this article.
August 3, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28771030/antibody-and-antibody-mimetic-immunotherapeutics
#20
Angeline N Ta, Brian R McNaughton
No abstract text is available yet for this article.
August 3, 2017: Future Medicinal Chemistry
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