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So Masaki et al.
Bioorganic & medicinal chemistry, 23(15), 4434-4441 (2015-07-07)
Dysregulation of dual-specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) has been demonstrated in several pathological conditions, including Alzheimer's disease and cancer progression. It has been recently reported that a gain of function-mutation in the human DYRK1B gene exacerbates metabolic syndrome by enhancing
Anil K Gorle et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 21(29), 10472-10481 (2015-06-05)
Ruthenium(II) complexes containing the tetradentate ligand bis[4(4'-methyl-2,2'-bipyridyl)]-1,n-alkane ("bbn "; n=10 and 12) have been synthesised and their geometric isomers separated. All [Ru(phen)(bbn )](2+) (phen=1,10-phenanthroline) complexes exhibited excellent activity against Gram-positive bacteria, but only the cis-α-[Ru(phen)(bb12 )](2+) species showed good activity
F Kazazi-Hyseni et al.
International journal of pharmaceutics, 482(1-2), 99-109 (2014-12-17)
Poly(D,L-lactic-co-hydroxymethyl glycolic acid) (PLHMGA) is a biodegradable copolymer with potential as a novel carrier in polymeric drug delivery systems. In this study, the biocompatibility of PLHMGA microspheres (PLHMGA-ms) was investigated both in vitro in three different cell types (PK-84, HK-2
Eveline Dischkaln Stolz et al.
The Journal of pharmacy and pharmacology, 66(12), 1774-1785 (2014-08-15)
Investigate the involvement of monoaminergic and glutamatergic systems on the antinociceptive and ataxic effects of uliginosin B, which we have already demonstrated to be a promising molecular scaffold to develop new analgesic drugs. Uliginosin B was obtained from hexane extract
Arun A Yadav et al.
Bioorganic & medicinal chemistry, 23(13), 3542-3551 (2015-04-30)
Drugs that target DNA topoisomerase II, such as the epipodophyllotoxin etoposide, are a clinically important class of anticancer agents. A recently published X-ray structure of a ternary complex of etoposide, cleaved DNA and topoisomerase IIβ showed that the two intercalated
Carina S D Wink et al.
Analytical and bioanalytical chemistry, 407(6), 1545-1557 (2015-01-13)
Lefetamine (N,N-dimethyl-1,2-diphenylethylamine, L-SPA) was marketed as an opioid analgesic in Japan and Italy. After being widely abused, it became a controlled substance. It seems to be a pharmaceutical lead for designer drugs because N-ethyl-1,2-diphenylethylamine (NEDPA) and N-iso-propyl-1,2-diphenylethylamine (NPDPA) were confiscated
Marco Evidente et al.
Chirality, 27(9), 557-562 (2015-05-27)
A new 3-substituted-5-diazenylcyclopentendione named kongiidiazadione was isolated from culture filtrates of Diaporthe kongii, associated with stem cankers on sunflower in Australia. Kongiidiazadione was characterized by spectroscopic (essentially nuclear magnetic resonance [NMR] and high-resolution, electrospray ionization, mass spectrometry [HRESIMS]) methods as
Ann Kathrin Strunz et al.
Bioorganic & medicinal chemistry, 23(14), 4034-4049 (2015-03-15)
Activation of chemokine CC receptors subtype 2 (CCR2) plays an important role in chronic inflammatory processes such as atherosclerosis, multiple sclerosis and rheumatoid arthritis. A diverse set of spirocyclic butanamides 4 (N-benzyl-4-(3,4-dihydrospiro[[2]benzopyran-1,4'-piperidin]-1'-yl)butanamides) was prepared by different combination of spirocyclic piperidines
Giuseppe Impallomeni et al.
Rapid communications in mass spectrometry : RCM, 29(9), 811-820 (2015-09-18)
Bacterial poly(3-hydroxyalkanoates) (PHAs) are an emergent class of plastic materials available from renewable resources. Their properties are strictly correlated with the comonomeric composition and sequence, which may be determined by various mass spectrometry approaches. In this paper we compare fast-atom
Abuzer Ali et al.
Natural product research, 29(14), 1307-1314 (2015-02-13)
The fruits of Withania coagulans Dunal (family: Solanaceae) are sweet, sedative, emetic, alterative and diuretic; used to treat asthma, biliousness, strangury, wounds, dyspepsia, flatulent colic, liver complaints and intestinal infections in the indigenous system of medicine. Phytochemical investigation of the
Yukiko Tsuji et al.
Plant biotechnology journal, 13(6), 821-832 (2015-01-13)
Bacteria-derived enzymes that can modify specific lignin substructures are potential targets to engineer plants for better biomass processability. The Gram-negative bacterium Sphingobium sp. SYK-6 possesses a Cα-dehydrogenase (LigD) enzyme that has been shown to oxidize the α-hydroxy functionalities in β-O-4-linked
Vijay Pawar et al.
Drug delivery, 22(3), 359-366 (2014-03-29)
The aim of this work was to prepare salts of 6-methoxy-2-naphthylacetic acid (6-MNA) to improve its physicochemical properties for percutaneous application. 6-MNA, an active metabolite of non-steroidal anti-inflammatory drug nabumetone has long half life and has the tendency to penetrate
Safinaz E-S Abbas et al.
Chemical biology & drug design, 85(5), 608-622 (2014-10-17)
Four series of some 4-substituted-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine derivatives 5a-f, 6a-f, 8a-f, and 9a-f were designed to be screened for their antitumor activity. All compounds were evaluated against breast (MCF-7) and lung (A-549) cell lines. Six compounds 5a, 5b, 6b, 6e, 9e, and
Nicholas G Davey et al.
Rapid communications in mass spectrometry : RCM, 29(23), 2187-2194 (2015-11-03)
The ability of membrane introduction mass spectrometry to quantitatively resolve low molecular weight volatile organic compounds (VOCs) such as benzene, toluene, ethylbenzene and xylene (BTEX) using electron ionization (EI) can be compromised by isobaric interferences. This work focuses on reducing
Jinyun Dong et al.
Bioorganic & medicinal chemistry, 22(24), 6876-6884 (2014-12-04)
Bcr-Abl plays an essential role in the pathogenesis and development of chronic myeloid leukaemia (CML). Inhibition of Bcr-Abl has great potential for therapeutic intervention in CML. In order to obtain novel and potent Bcr-Abl inhibitors, twenty seven 4,6-disubstituted pyrimidines were
H Yockell-Lelièvre et al.
The Analyst, 140(15), 5105-5111 (2015-06-03)
The ability to detect small molecules in a rapid and sensitive manner is of great importance in the field of clinical chemistry, and the advancement of novel biosensors is key to realising point-of-care analysis for essential targets. Testosterone is an
A John Blacker et al.
Beilstein journal of organic chemistry, 11, 2408-2417 (2016-01-07)
The continuous flow synthesis of a range of organic solutions of N,N-dialkyl-N-chloramines is described using either a bespoke meso-scale tubular reactor with static mixers or a continuous stirred tank reactor. Both reactors promote the efficient mixing of a biphasic solution
Qi-Hui Zhang et al.
Journal of Asian natural products research, 17(5), 497-503 (2015-03-24)
Two new secondary metabolites, (2S)-5-acetamidopentyl-2-hydroxypropanoate (1) and 2, 5, 7-trihydroxy-4-(3'-methylbut-2'-en-1'-yl) oxy-2H-naphtho [1, 8-b c] furan-9-one (2) were isolated from the marine-derived fungus Nigrospora sphaerica. The structures were established on the basis of their spectroscopic data, including 1D NMR and 2D
Bo Wu et al.
Nature communications, 6, 6468-6468 (2015-03-04)
The endohedral fullerenes lead to well-protected internal species by the fullerene cages, and even highly reactive radicals can be stabilized. However, the manipulation of the magnetic properties of these radicals from outside remains challenging. Here we report a system of
Gianluca Gilardoni et al.
Chemistry & biodiversity, 12(6), 946-954 (2015-06-18)
Coussarea macrophylla (Mart.) Müll.Arg. (Rubiaceae) was collected in Ecuador, and the bark was extracted with AcOEt. Chromatographic separation afforded six novel 3,4-secocycloartane and 3,4-secodammarane triterpenes, named macrocoussaric acids A-F, together with the known metabolites secaubryenol and 3,4-secodammara-4(28),20,24-triene-3,26-dioic acid. The structures
Paulina Maksym-Bębenek et al.
Macromolecular bioscience, 15(11), 1616-1624 (2015-07-23)
The core-shell micelles in aqueous solutions were prepared at low CAC values (<0.1 mg · mL(-1) ) from amphiphilic graft copolymers consisting of poly(methyl methacrylate) backbone (120-165 units) with loosely grafted (17-40%) hydroxyl-capped PEG (9 vs 6 units in side chain) for drug
E Mázl Chánová et al.
Physiological research, 64 Suppl 1, S61-S73 (2015-10-09)
In this study, we investigate the preparation of surface pattern of functional groups on poly(lactide) (PLA) surfaces through the controlled deposition of core-shell self-assemblies based on functionalized PLA-b-PEO amphiphilic block copolymers from selective solvents. Through grafting RGDS peptide onto the
Satoru Matsukawa et al.
Molecules (Basel, Switzerland), 20(10), 18482-18495 (2015-10-17)
The ring-opening of N-tosylaziridines with various acid anhydrides catalyzed by 5 mol % of 1,5,7-triazabicyclo[4,4,0]dec-5-ene (TBD) afforded the corresponding β-amino esters in excellent yields under mild reaction conditions. Polymer-supported catalyst, PS-TBD also acts as a good catalyst for this reaction.
Zhi-Pei Sang et al.
Chemical biology & drug design, 86(5), 1168-1177 (2015-05-06)
A series of scutellarein carbamate derivatives were designed and synthesized based on the multitarget-directed drug design strategy for treatment of Alzheimer's disease. Their acetylcholinesterase and butyrylcholinesterase inhibitory activities, antioxidant activities, metals chelation, and neuroprotective effects against hydrogen peroxide-induced PC12 cell
Ogbole Omonike Oluyemisi et al.
Pharmaceutical biology, 53(6), 882-887 (2014-11-29)
Plants of the Zephyranthes genus are globally used in folk medicine. In a previous study, Zephyranthes candida Linn. (Amaryllidaceae) was identified as having antiviral properties; this led to anti-poliovirus assay-guided isolation of compounds from crude methanol extract of the plant.
Thomas J Farmer et al.
International journal of molecular sciences, 16(7), 14912-14932 (2015-07-07)
Utilisation of bio-derived platform molecules in polymer synthesis has advantages which are, broadly, twofold; to digress from crude oil dependence of the polymer industry and secondly to reduce the environmental impact of the polymer synthesis through the inherent functionality of
Piers R J Gaffney et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 21(26), 9535-9543 (2015-05-28)
Due to the discovery of RNAi, oligonucleotides (oligos) have re-emerged as a major pharmaceutical target that may soon be required in ton quantities. However, it is questionable whether solid-phase oligo synthesis (SPOS) methods can provide a scalable synthesis. Liquid-phase oligo
Paul D Boudreau et al.
PloS one, 10(7), e0133297-e0133297 (2015-07-30)
Moorea producens JHB, a Jamaican strain of tropical filamentous marine cyanobacteria, has been extensively studied by traditional natural products techniques. These previous bioassay and structure guided isolations led to the discovery of two exciting classes of natural products, hectochlorin (1)
Dragana Stevanović et al.
Carbohydrate research, 407, 111-121 (2015-03-10)
In situ generated zirconium catalyst from a sacrificial zirconium anode was successfully applied to promote Ferrier rearrangement of 3,4,5-tri-O-acetyl-D-glucal and 6-deoxy-3,4-di-O-acetyl-L-glucal (3,4-di-O-acetyl-L-rhamnal) in the presence of three thiols and eleven thiophenols as nucleophiles. A simple constant current electrolysis (20 mA
Jun Cao et al.
International journal of pharmaceutics, 471(1-2), 28-36 (2014-05-20)
A novel pH-sensitive polymeric micelle was reported. Methoxy poly(ethylene glycol)-b-poly(ϵ-caprolactone) copolymer with citraconic amide as pH-sensitive bond was synthesized (mPEG-pH-PCL). The copolymers self-assembled into micelles to encapsulate anticancer drug doxorubicin (DOX). The morphology, size and size distribution, drug release profile
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