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https://www.readbyqxmd.com/read/28937776/4-c-methoxy-2-deoxy-2-fluoro-modified-ribonucleotides-improve-metabolic-stability-and-elicit-efficient-rnai-mediated-gene-silencing
#1
Elise Malek-Adamian, Dale Guenther, Shigeo Matsuda, Saúl Martínez-Montero, Ivan Zlatev, Joel Harp, Mihai Burai Patrascu, Donald J Foster, Johans J Fakhoury, Lydia Perkins, Nicolas Moitessier, Rajar Manoharan, Nate Taneja, Anna Bisbe, Klaus Charisse, Martin A Maier, Kallanthottathil G Rajeev, Martin Egli, Muthiah Manoharan, Masad J Damha
We designed novel 4'-modified 2'-deoxy-2'-fluorouridine (2'-F U) analogues with the aim to improve nuclease resistance and potency of therapeutic siRNAs by introducing 4'-C-methoxy (4'-OMe) as the alpha (C4'α) or beta (C4'β) epimers. The C4'α epimer was synthesized by a stereoselective route in six steps; however, both α and β epimers could be obtained by a non-stereoselective approach starting from 2'-F U. (1)H-NMR analysis and computational investigation of the α-epimer revealed that the 4'-OMe imparts a conformational bias towards the North-East sugar pucker, due to intramolecular hydrogen bonding and hyperconjugation effects...
September 22, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28936596/age-related-behavioral-morphological-and-physiological-changes-in-the-hippocampus-of-zitter-rats
#2
Ayuka Ehara, Masao Maekawa, Yuuichi Hori, Kazuhiko Nakadate, Shiuchi Ueda
Convulsive seizure is known to be associated with hippocampal abnormalities, such as hilar cell degeneration, abnormal mossy fiber sprouting in the dentate gyrus (DG) and abnormal expression of immediate early genes. However, whether these morphological changes are a cause or consequence of convulsive seizures has remained contentious. Zitter (zi/zi) rats carry a mutation of the attractin gene and display spongiform degeneration of the brain. Spontaneous convulsive seizures in zi/zi rats over 8 months (M) old were demonstrated using 24-h video monitoring...
September 21, 2017: Anatomical Science International
https://www.readbyqxmd.com/read/28936429/clinical-pet-mri-in-neurooncology-opportunities-and-challenges-from-a-single-institution-perspective
#3
REVIEW
Lisbeth Marner, Otto M Henriksen, Michael Lundemann, Vibeke Andrée Larsen, Ian Law
PURPOSE: Magnetic resonance imaging (MRI) plays a key role in neurooncology, i.e., for diagnosis, treatment evaluation and detection of recurrence. However, standard MRI cannot always separate malignant tissue from other pathologies or treatment-induced changes. Advanced MRI techniques such as diffusion-weighted imaging, perfusion imaging and spectroscopy show promising results in discriminating malignant from benign lesions. Further, supplemental imaging with amino acid positron emission tomography (PET) has been shown to increase accuracy significantly and is used routinely at an increasing number of sites...
2017: Clinical and Translational Imaging: Reviews in Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/28935562/n-2-methoxyphenyl-benzenesulfonamide-a-novel-regulator-of-neuronal-g-protein-gated-inward-rectifier-k-channels
#4
Kenneth B Walsh, Elaine A Gay, Bruce E Blough, David W Geurkink
G protein-gated inward rectifier K(+) (GIRK) channels are members of the super-family of proteins known as inward rectifier K(+) (Kir) channels and are expressed throughout the peripheral and central nervous systems. Neuronal GIRK channels are the downstream targets of a number of neuromodulators including opioids, somatostatin, dopamine and cannabinoids. Previous studies have demonstrated that the ATP-sensitive K(+) channel, another member of the Kir channel family, is regulated by sulfonamide drugs. Therefore, to determine if sulfonamides also modulate GIRK channels, we screened a library of arylsulfonamide compounds using a GIRK channel fluorescent assay that utilized pituitary AtT20 cells expressing GIRK channels along with the somatostatin type-2 and -5 receptors...
September 18, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28932469/ethyl-2-amino-1-4-fluoro-phen-yl-5-oxo-4-5-di-hydro-1h-pyrrole-3-carboxyl-ate-crystal-structure-and-hirshfeld-surface-analysis
#5
U H Patel, Chintan Jotaniya, D A Shah, Bhavesh Socha
In the title mol-ecule, C12H13FN2O3, the central pyrrole ring makes a dihedral angle of 9.2 (3)° with the eth-oxy carbonyl moiety whereas the fluoro-phenyl ring is rotated by 67.6 (2)° from the pyrrole ring. Supra-molecular aggregation is due to off-centric π-π stacking inter-actions involving screw-related pairs of mol-ecules, which are further connected by N-H⋯O and C-H⋯O inter-actions, forming a sinusoidal pattern along the [001] direction on the bc plane. Three-dimensional Hirshfeld surface analysis and two-dimensional fingerprint plots confirm the contributions of these inter-actions...
September 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28932463/crystal-structure-of-penoxsulam
#6
Hyunjin Park, Jineun Kim, Hojae Chiang, Tae Ho Kim
The title compound, C16H14F5N5O5S [systematic name: 2-(2,2-di-fluoro-eth-oxy)-N-(5,8-dimeth-oxy-1,2,4-triazolo[1,5-c]pyrimidin-2-yl)-6-(tri-fluoro-meth-yl)benzene-sulfonamide], is used as a herbicide. The asymmetric unit of this structure comprises two independent mol-ecules, A and B. The dihedral angles between the ring planes of the triazolo-pyrimidine ring systems and the benzene rings are 68.84 (7)° for A and 68.05 (6)° for B. In the crystal, weak inter-molecular π-π inter-actions, with centroid-centroid separations of 3...
September 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28932437/coordination-compounds-containing-bis-di-thiol-ene-chelated-molybdenum-iv-and-oxalate-comparison-of-terminal-with-bridging-oxalate
#7
Agata Gapinska, Alan J Lough, Ulrich Fekl
Two coordination compounds containing tetra-n-butyl-ammonium cations and bis-tfd-chelated molybdenum(IV) [tfd(2-) = S2C2(CF3)2(2-)] and oxalate (ox(2-), C2O4(2-)) in complex anions are reported, namely bis-(tetra-n-butyl-ammonium) bis-(1,1,1,4,4,4-hexa-fluoro-but-2-ene-2,3-di-thiol-ato)oxalatomolybdate(IV)-chloro-form-oxalic acid (1/1/1), (C16H36N)2[Mo(C4F6S2)2(C2O4)]·CHCl3·C2H2O4 or (N (n) Bu4)2[Mo(tfd)2(ox)]·CHCl3·C2H2O4, and bis-(tetra-n-butyl-ammonium) μ-oxalato-bis-[bis-(1,1,1,4,4,4-hexa-fluoro-but-2-ene-2,3-di-thiol-ato)molybdate(IV)], (C16H36N)2[Mo2(C4F6S2)4(C2O4)] or (N (n) Bu4)2[(tfd)2Mo(μ-ox)Mo(tfd)2]...
July 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28932426/crystal-structure-of-e-n-3-fluoro-2-hy-droxy-benzyl-idene-isonicotinohydrazide
#8
Suwadee Jiajaroen, Kittipong Chainok, Filip Kielar
In the title compound, C13H10FN3O2, the mol-ecule has an E conformation with respect to the C=N bond of the hydrazone bridge. The dihedral angle between the isonicotinoyl and fluoro-phenol moieties is 4.03 (4)°, and an intra-molecular O-H⋯N hydrogen bond generates an S(6) ring motif. In the crystal, mol-ecules are linked by N-H⋯N and C-H⋯N hydrogen bonds, forming chains propagating along the a-axis direction. The chains are linked by C-H⋯O hydrogen bonds, resulting in the formation of layers lying parallel to the ab plane...
July 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28932423/crystal-structure-of-triphenylphosphonium-meth-yl-enetrifluoroborate
#9
Christopher M Bateman, Lev N Zakharov, Eric R Abbey
The title compound, C19H17BF3P {alternative name: triphen-yl[(tri-fluoro-boran-yl)meth-yl]phosphanium}, was formed by the reaction of tri-phenyl-phosphine with potassium iodo-methyl-tri-fluoro-borate. The mol-ecule features a nearly staggered conformation along the P-C bond and a less than staggered conformation along the C-B bond. In the crystal, weak C-H⋯F hydrogen bonds between the meta-phenyl C-H groups and the tri-fluoro-borate B-F groups form chains of R2(2)(16) rings along [100]. These chains are are further stabilized by weak C-H⋯π inter-actions...
July 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28932422/syntheses-and-crystal-structures-of-two-adamantyl-substituted-1-2-4-triazole-5-thione-n-mannich-bases
#10
Monirah A Al-Alshaikh, Aamal A Al-Mutairi, Hazem A Ghabbour, Ali A El-Emam, Mohammed S M Abdelbaky, Santiago Garcia-Granda
In the title N-Mannich bases, 3-(adamantan-1-yl)-4-(4-fluoro-phen-yl)-1-[(4-phenyl-piperazin-1-yl)meth-yl]-4,5-di-hydro-1H-1,2,4-triazole-5-thione (C29H34FN5S) (I), and 3-(adamantan-1-yl)-4-(4-fluoro-phen-yl)-1-{[4-(2-meth-oxyphen-yl)piperazin-1-yl]-meth-yl}-4,5-di-hydro-1H-1,2,4-triazole-5-thione (C30H36FN5OS) (II), fluoro-phenyl, adamantane and piperazine moieties are linked to a planar triazole ring. There is an additional phenyl ring on the piperazine ring in (I) and a meth-oxy-phenyl ring in (II). In compound (I), the fluoro-phenyl and phenyl rings are inclined to the triazole ring by 86...
July 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28932421/structure-of-7-hy-droxy-3-2-meth-oxy-phen-yl-2-tri-fluoro-meth-yl-4h-chromen-4-one
#11
John Nicolson Low, Ligia R Gomes, Alexandra Gaspar, Fernanda Borges
Herein, the synthesis and crystal structure of 7-hy-droxy-3-(2-meth-oxy-phen-yl)-2-tri-fluoro-meth-yl-4H-chromen-4-one, C17H11F3O4, are reported. This isoflavone is used as a starting material in the preparation an array of potent and competitive FPR antagonists. The pyran ring significantly deviates from planarity and the dihedral angle between the benzo-pyran mean plane and that of the exocyclic benzene ring is 88.18 (4)°. In the crystal, O-H⋯O hydrogen bonds connect the mol-ecules into C(8) chains propagating in the [010] direction...
July 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28931302/learning-metabolic-brain-networks-in-mci-and-ad-by-robustness-and-leave-one-out-analysis-an-fdg-pet-study
#12
Zhijun Yao, Bin Hu, Xuejiao Chen, Yuanwei Xie, Jürg Gutknecht, Dennis Majoe
This study attempted to better understand the properties associated with the metabolic brain network in mild cognitive impairment (MCI) and Alzheimer's disease (AD). Graph theory was employed to investigate the topological organization of metabolic brain network among 86 patients with MCI, 89 patients with AD, and 97 normal controls (NCs) using 18F fluoro-deoxy-glucose positron emission tomography (FDG-PET) data. The whole brain was divided into 82 areas by Brodmann atlas to construct networks. We found that MCI and AD showed a loss of small-world properties and topological aberrations, and MCI showed an intermediate measurement between NC and AD...
January 1, 2017: American Journal of Alzheimer's Disease and Other Dementias
https://www.readbyqxmd.com/read/28931276/the-stereoselective-synthesis-of-pyrrolidines-containing-3-fluoro-quaternary-stereocenter-via-copper-i-catalyzed-asymmetric-1-3-dipolar-cycloaddition
#13
Yang-Zi Liu, Shao-Jing Shang, Wu-Lin Yang, Xiaoyan Luo, Wei-Ping Deng
A highly efficient asymmetric 1,3-dipolar cycloaddition of azomethine ylides to β,β-disubstituted β-fluoro-acrylates catalyzed by a chiral N,O-ligand/Cu(CH3CN)4BF4 system is reported, affording chiral densely-substituted pyrrolidines with four contiguous stereocenters, including one fluorinated quaternary stereocenter at the 3-position, in good to excellent yields (up to 99%), with excellent levels of diastereo- and enantioselectivities (dr >20:1; ee up to 99%).
September 21, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28930474/unveiling-the-self-assembling-behavior-of-5-fluorouracil-and-its-n-n-dimethyl-derivative-a-spectroscopic-and-microscopic-approach
#14
Pavel Banerjee, Devdeep Mukherjee, Tapas Kumar Maiti, Nilmoni Sarkar
At physiological conditions, 5-fluorouracil (5-FU), an anti-cancer drug self-assembles into fibrils by strong hydrogen bonding network while its methylated derivative, 5-fluoro-1,3-dimethyluracil (5-FDMU) do not make fibril due to lack of strong hydrogen bonding motif. In vitro, 5-FU self-assembly is sensitive to physicochemical conditions like the pH and ionic strength of the solution, which tune the strength of the non-covalent driving forces. Here we report a surprising finding that the buffer-which is necessary to control the pH and is typically considered to be inert-also significantly, influences 5-FU self-assembly which indicates an important role of counter-ions in the fibril formation...
September 20, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28927903/linker-structure-activity-relationships-in-fluorodeoxyglucose-chlorambucil-conjugates-for-tumor-targeted-chemotherapy
#15
Mostafa El Hilali, Bastien Reux, Eric Debiton, Fernand Leal, Marie-Josephe Galmier, Magali Vivier, Jean-Michel Chezal, Elisabeth Miot-Noirault, Pascal Coudert, Valérie Weber
Nitrogen mustards, such as chlorambucil (CLB), can cause adverse side-effects due to ubiquitous distribution in non-target organs. To minimize this toxicity, strategies of tumor-targeting drug delivery have been developed, where a cytotoxic warhead is linked to a tumor-cell-specific small ligand. Malignant cells exhibit marked glucose avidity and an accelerated metabolism by aerobic glycolysis, known as the Warburg effect, and recognized as a hallmark of cancer. A targeting approach exploiting the Warburg effect by conjugation of CLB to 2-fluoro-2-deoxyglucose (FDG) was previously reported and identified two peracetylated glucoconjugates 2 and 3 with promising antitumor activities in vivo...
August 30, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28927790/design-semisynthesis-and-potent-cytotoxic-activity-of-novel-10-fluorocamptothecin-derivatives
#16
Cheng-Jie Yang, Zi-Long Song, Masuo Goto, Pei-Ling Hsu, Xiao-Shuai Zhang, Qian-Ru Yang, Ying-Qian Liu, Mei-Juan Wang, Susan L Morris-Natschke, Xiao-Fei Shang, Kuo-Hsiung Lee
Fluorination is a well-known strategy for improving the bioavailability of bioactive molecules in the lead optimization phase of drug discovery projects. In an attempt to improve the antitumor activity of camptothecins (CPTs), novel 10-fluoro-CPT derivatives were designed, synthesized and evaluated for cytotoxicity against five human cancer cell lines (A-549, MDA-MB-231, KB, KB-VIN and MCF-7). All of the derivatives showed more potent in vitro cytotoxic activity than the clinical CPT-derived drug irinotecan against the tumor cell lines tested, and most of them showed comparable or superior potency to topotecan...
September 8, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28927125/benign-metastasizing-leiomyoma-and-18-fdg-pet-ct-a-case-report-and-literature-review
#17
Yusuke Sawai, Toshiki Shimizu, Yuta Yamanaka, Maiko Niki, Shosaku Nomura
Pulmonary benign metastasizing leiomyoma (PBML) is a rare disease entity that usually occurs in females of reproductive age with a previous history of uterine myoma. It is typically characterized by multiple pulmonary tumors consisting of benign leiomyoma cells. In the present study, two cases of PBML are discussed. The patient in each case underwent 2-deoxy-2-(fluorine-18)-fluoro-D-glucose positron emission tomography/computed tomography (18-FDG-PET/CT) scans. One patient demonstrated a lack of 18-FDG uptake and a quiescent clinical course...
September 2017: Oncology Letters
https://www.readbyqxmd.com/read/28927093/detailed-analysis-of-a-superficial-cd34-positive-fibroblastic-tumor-a-case-report-and-review-of-the-literature
#18
Kensaku Yamaga, Akihiro Fujita, Mari Osaki, Satoshi Kuwamoto, Naoko Ishiguro, Tadahito Yamamoto, Hideki Nagashima
Superficial cluster of differentiation (CD)34-positive fibroblastic tumor (SCPFT) is a rare mesenchymal neoplasm of borderline malignancy. It is characterized by a superficial location, marked cellular pleomorphism, an extremely low incidence of mitotic figures, and strong CD34 immunohistochemical positivity. As SCPFT is a recently described neoplasm, its characteristics are yet to be fully elucidated. To the best of our knowledge, no detailed studies regarding the imaging findings and cytogenetic analyses of SCPFTs exist...
September 2017: Oncology Letters
https://www.readbyqxmd.com/read/28927061/5fu-resistance-caused-by-reduced-fluoro-deoxyuridine-monophosphate-and-its-reversal-using-deoxyuridine
#19
Ryutaro Mori, Manabu Futamura, Toshiyuki Tanahashi, Yoshihiro Tanaka, Nobuhisha Matsuhashi, Kazuya Yamaguchi, Kazuhiro Yoshida
The mechanism of 5-fluorouracil (5FU) resistance was investigated, focusing on the level of thymidylate synthase (TS) ternary complex formed with fluoro-deoxyuridine monophosphate (FdUMP). MKN45 and 5FU-resistant MKN45/F2R cells were treated with 5FU and fluoro-deoxyuridine (FdU) in combination with deoxyuridine (dU) and thymidine (dT). Subsequently, the levels of ternary complex were determined by western blotting and the cell viability was calculated using an MTT assay. MKN45/F2R cells exhibited 5FU resistance (56...
September 2017: Oncology Letters
https://www.readbyqxmd.com/read/28925503/quantitative-analysis-of-mouse-dural-afferent-neurons-expressing-trpm8-vglut3-and-nf200
#20
Lynn Ren, Michelle Jaehee Chang, Zhiyu Zhang, Ajay Dhaka, Zhaohua Guo, Yu-Qing Cao
OBJECTIVE: To quantify the abundance of dural afferent neurons expressing transient receptor potential channel melastatin 8 (TRPM8), vesicular glutamate transporter 3 (VGLUT3), and neurofilament 200 (NF200) in adult mice. BACKGROUND: With the increasing use of mice as a model system to study headache mechanisms, it is important to understand the composition of dural afferent neurons in mice. In a previous study, we have measured the abundance of mouse dural afferent neurons that express neuropeptide calcitonin gene-related peptide as well as two TRP channels TRPV1 and TRPA1, respectively...
September 19, 2017: Headache
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