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Showing 1-30 of 272 results for "151823" within Papers
Ryuji Uchida et al.
The Journal of antibiotics, 67(11), 777-781 (2014-06-12)
A small molecule named habiterpenol produced by actinomycete Phytohabitans suffuscus 3787_5 was found to abrogate bleomycin-induced G2 arrest in Jurkat cells. Habiterpenol showed no cytotoxic effect on Jurkat cells even at 273 μM; however, the compound inhibited bleomycin-induced G2 arrest in
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
Tuomas Mehtiö et al.
Carbohydrate research, 402, 102-110 (2014-12-17)
A series of copolyanhydrides, consisting of 2,3,4,5-tetra-O-acetylgalactaric acid (AGA) and adipic acid (AA) as monomer units, was polymerized. Synthesis of AGA monomer consisted of two steps. First, O-acetylation of galactaric acid secondary hydroxyl groups was performed using acetic anhydride as
Virsinha Reddy et al.
Organic & biomolecular chemistry, 13(12), 3732-3741 (2015-02-18)
An efficient and mild protocol for the direct construction of aryl- and alkyl-substituted isoquinolines has been realized through silver nitrate catalyzed aromatic annulation of o-(1-alkynyl)arylaldehydes and ketones with ammonium acetate. The salient feature of this methodology is that this annulation
Yasuhiro Shimamoto et al.
Bioorganic & medicinal chemistry, 23(4), 876-890 (2015-01-24)
The design and evaluation of a novel decahydroisoquinolin scaffold as an inhibitor for severe acute respiratory syndrome (SARS) chymotrypsin-like protease (3CL(pro)) are described. Focusing on hydrophobic interactions at the S2 site, the decahydroisoquinolin scaffold was designed by connecting the P2
Bhakti B Salgaonkar et al.
International journal of biological macromolecules, 78, 339-346 (2015-04-22)
Polyhydroxyalkanoates (PHA's) can be a key solution for pollution problems caused by plastics derived from petrochemical sources. Extremely halophilic archaeon Halogeometricum borinquense strain E3 showed maximum PHA accumulation of 73.51 ±1.7% (wt/wt) of cell dry weight (CDW) with 2% glucose.
Vladimir E Oslovsky et al.
Nucleosides, nucleotides & nucleic acids, 34(7), 475-499 (2015-07-15)
Several methods for the preparation of some N(6)-substituted adenosines based on selective 1-N-alkylation with subsequent Dimroth rearrangement were developed. The proposed methods seem to be effective for the preparation of natural N(6)-isopentenyl- and N(6)-benzyladenosines, which are known to possess pronounced
Ho-Joong Kim et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 21(33), 11836-11842 (2015-07-07)
Threefold symmetric rigid-core molecules with an internally grafted poly(ethylene oxide) (PEO) chain were synthesized, and their self-assembled structures were characterized using differential scanning calorimetry, TEM, and 1D and 2D X-ray scatterings in the solid state. The tripod compounds based on
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
Raj Kumar Roy et al.
Nature communications, 6, 7237-7237 (2015-05-27)
Biopolymers such as DNA store information in their chains using controlled sequences of monomers. Here we describe a non-natural information-containing macromolecule that can store and retrieve digital information. Monodisperse sequence-encoded poly(alkoxyamine amide)s were synthesized using an iterative strategy employing two
Phuong Hoang Tran et al.
Molecules (Basel, Switzerland), 20(10), 19605-19619 (2015-10-31)
A fast and green method is developed for regioselective acylation of indoles in the 3-position without the need for protection of the NH position. The method is based on Friedel-Crafts acylation using acid anhydrides. The method has been optimized, and
Francesco Russo et al.
ChemistryOpen, 4(3), 342-362 (2015-08-08)
This is the first report of 5-styryl-oxathiazol-2-ones as inhibitors of the Mycobacterium tuberculosis (Mtb) proteasome. As part of the study, the structure-activity relationship of oxathiazolones as Mtb proteasome inhibitors has been investigated. Furthermore, the prepared compounds displayed a good selectivity
Four new cembranoids from the soft coral Sarcophyton sp.
Zhong-Bin Cheng et al.
Magnetic resonance in chemistry : MRC, 52(9), 515-520 (2014-07-22)
Loredana Leone et al.
ChemistryOpen, 4(3), 370-377 (2015-08-08)
Current molecular cryptography (MoCryp) systems are almost exclusively based on DNA chemistry and reports of cryptography technologies based on other less complex chemical systems are lacking. We describe herein, as proof of concept, the prototype of the first asymmetric MoCryp
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