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https://www.readbyqxmd.com/read/27187857/synthesis-and-biological-evaluation-of-4-2-fluorophenoxy-3-3-bipyridine-derivatives-as-potential-c-met-inhibitors
#1
Sijia Zhao, Yu Zhang, Hongyang Zhou, Shuancheng Xi, Bin Zou, Guanglong Bao, Limei Wang, Jiao Wang, Tianfang Zeng, Ping Gong, Xin Zhai
Six series of novel 4-(2-fluorophenoxy)-3,3'-bipyridine derivatives conjugated with aza-aryl formamide/amine scaffords were designed and synthesized through a structure-based molecular hybridization approach. The target compounds were evaluated for c-Met kinase inhibitory activities and cytotoxicity against four cancer cell lines (HT-29, A549, MKN-45 and MDA-MB-231) in vitro. Most compounds exhibited moderate to excellent potency, and the most promising candidate 26c (c-Met kinase IC50 = 8.2 nM) showed a 4...
September 14, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/23634850/distance-dependence-of-intrahelix-ru-ii-to-os-ii-polypyridyl-excited-state-energy-transfer-in-oligoproline-assemblies
#2
M Kyle Brennaman, Cavan N Fleming, Cheryl A Slate, Scafford A Serron, Stephanie E Bettis, Bruce W Erickson, John M Papanikolas, Thomas J Meyer
Energy transfer between the metal-to-ligand charge transfer (MLCT) excited states of [Pra [M(II)(bpy)2(4-Me-4'(-N(H)CO)bpy)](PF6)2 units ([Pra(M(II)bpy2(mbpy)](2+): M(II) = Ru(II) or Os(II), bpy = 2,2'-bipyridine, mbpy = 4'-methyl-2,2'-bipyridine-4-carboxamido, Pra = 4-M(II)-L-proline) linked covalently to oligoproline assemblies in room temperature acetonitrile occurs on the picosecond-nanosecond time scale and has been time-resolved by transient emission measurements. Three derivatized oligoprolines, [CH3-CO-Pro6-Pra[Os(II)(bpy)2(mbpy)](2+)-Pro2-Pra[Ru(II)(bpy)2(mbpy)](2+)-Pro2-Pra[Ru(II)(bpy)2(mbpy)](2+)-Pro6-Glu-NH2](6+) (ORR-2, Pro = L-proline and Glu = glutamic acid); [CH3-CO-Pro6-Pra[Os(II)(bpy)2(mbpy)](2+)-Pro3-Pra[Ru(II)(bpy)2(mbpy)](2+)-Pro3-Pra[Ru(II)(bpy)2(mbpy)](2+)-Pro6-Glu-NH2](6+) (ORR-3); and CH3-CO-Pro6-Pra[Os(II)(bpy)2(mbpy)](2+)-Pro5-Pra[Ru(II)(bpy)2(mbpy)](2+)-Pro5-Pra[Ru(II)(bpy)2(mbpy)](2+)Pro6-Glu2-NH2](6+) (ORR-5), were prepared by using solid-phase peptide synthesis...
May 30, 2013: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/21402432/optimization-of-3-phenylthio-quinolinium-compounds-against-opportunistic-fungal-pathogens
#3
Comfort A Boateng, Xue Y Zhu, Melissa R Jacob, Shabana I Khan, Larry A Walker, Seth Y Ablordeppey
Ring-opened benzothieno[3,2-b]quinolinium salts (3) were designed and synthesized with substitution on the thiophene moiety. In vitro screenings were carried out against fungal pathogens including Cryptococcus neoformans, Candida albicans, Candida glabrata, Candida krusei and Aspergillus fumigatus. In all, by replacing the N-methyl group (2) with N-ω-phenylpentyl or ω-cyclohexylpentyl group to form substituted 3-(phenylthio)quinolinium compounds produced remarkable potencies, as high as 300-fold (cf, cryptolepine (1)=250 μg/mL vs 11p=0...
May 2011: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/18072572/-ectopic-bone-induction-in-vivo-after-transplantation-of-skeletal-satellite-cells-from-green-fluorescence-protein-transgenic-mouse-transfected-by-adenoviral-vectors-encoding-bone-morphogenetic-protein-2
#4
Feng-he Zhang, Ping Huang, Feng-cai Wei, Shu-yang Sun
OBJECTIVE: To observe the ability of induced ectopic bone using skeletal muscles satellite cells (SMSCs) from newborn green fluorescence protein (GFP) transgenic mice mediated by Ad-BMP2. METHODS: Transplantation of SMSCs transduced with Ad-BMP2 into back lamb muscles of subfascia in wildtype 129sv mice with a complex of collagen scaffords, then the tissue histologic examination, X ray plain film, fluorescence microscopy were used. RESULTS: Transplantation of SMSCs transfected with Ad-BMP2 into back lamb muscles of subfascia generated ectopic bone formation involving GFP-positive osteoblasts and osteocytes 2 weeks and mature bone formation 4 weeks after transplantation...
October 2007: Hua Xi Kou Qiang Yi Xue za Zhi, Huaxi Kouqiang Yixue Zazhi, West China Journal of Stomatology
https://www.readbyqxmd.com/read/16808505/synthesis-and-characterization-of-oligoproline-based-molecular-assemblies-for-light-harvesting
#5
W Steven Aldridge, Brooks J Hornstein, Scafford Serron, Dana M Dattelbaum, Jon R Schoonover, Thomas J Meyer
Helical oligoproline arrays provide a structurally well-defined environment for building photochemical energy conversion assemblies. The use of solid-phase peptide synthesis (SPPS) to prepare four such arrays, consisting of 16, 17, 18, and 19 amino acid residues, is described here. Each array contains the chromophore [Rub'(2)m](PF(6))(2) (b' = 4,4'-diethylamidocarbonyl-2,2'-bipyridine; m = 4-methyl-2,2'-dipyridine-4'-carboxylic acid) and the electron transfer donor PTZ (phenothiazine). The arrays differ systematically in the distance between the redox-active metal complex and PTZ sites...
July 7, 2006: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/15762737/photoelectrochemistry-on-ru-ii-2-2-bipyridine-phosphonate-derivatized-tio2-with-the-i3-i-and-quinone-hydroquinone-relays-design-of-photoelectrochemical-synthesis-cells
#6
Laurie A Gallagher, Scafford A Serron, Xingu Wen, Brooks J Hornstein, D M Dattelbaum, J R Schoonover, Thomas J Meyer
Photocurrent measurements have been made on nanocrystalline TiO2 surfaces derivatized by adsorption of a catalyst precursor, [Ru(tpy)(bpy(PO3H2)2)(OH2)]2+, or chromophore, [Ru(bpy)2 (bpy(PO3H2)2)]2+ (tpy is 2,2':6',2' '-terpyridine, bpy is 2,2'-bipyridine, and bpy(PO3H2)2 is 2,2'-bipyridyl-4,4'-diphosphonic acid), and on surfaces containing both complexes. This is an extension of earlier work on an adsorbed assembly containing both catalyst and chromophore. The experiments were carried out with the I3-/I- or quinone/hydroquinone (Q/H2Q) relays in propylene carbonate, propylene carbonate-water mixtures, and acetonitrile-water mixtures...
March 21, 2005: Inorganic Chemistry
https://www.readbyqxmd.com/read/15521771/evidence-for-through-space-electron-transfer-in-the-distance-dependence-of-normal-and-inverted-electron-transfer-in-oligoproline-arrays
#7
Scafford A Serron, W Stephen Aldridge Iii, Cavan N Fleming, Ryan M Danell, Mu-Hyun Baik, Milan Sykora, Dana M Dattelbaum, Thomas J Meyer
Four new helical oligoproline assemblies containing 16, 17, 18, and 19 proline residues and ordered arrays of a Ru(II)-bipyridyl chromophore and a phenothiazine electron-transfer donor have been synthesized in a modular fashion by solid-phase peptide synthesis. These arrays are illustrated and abbreviated as CH(3)CO-Pro(6)-Pra(PTZ)-Pro(n)()-Pra(Ru(II)b(2)m)(2+)-Pro(6)-NH(2), where PTZ is 3-(10H-phenothiazine-10)propanoyl and (Ru(II)b'(2)m)(2+) is bis(4,4'-diethylamide-2,2'-bipyridine)(4-methyl,4'-carboxylate,2,2'-bipyridine)ruthenium(II) dication with n = 2 (2), 3 (3), 4 (4), and 5 (5)...
November 10, 2004: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/14614707/experimental-assessment-of-small-intestinal-submucosa-as-a-small-bowel-graft-in-a-rat-model
#8
Zhong Qiu Wang, Yasuhiro Watanabe, Akira Toki
BACKGROUND/PURPOSE: Small intestinal submucosa (SIS) is an extracellular matrix used in tissue engineering. The purpose of this study is to evaluate the feasibility of using SIS as a scafford for small bowel regeneration in a rat model. METHODS: A 2-cm length tubular SIS graft from donor Sprague Dawley rats was interposed with bilateral anastomosis in the median tract of an isolated ileal loop of Lewis rats used to construct an ileostomy. The grafts were harvested and analyzed at each of the time-points ranging from 2 weeks to 24 weeks after operation using histology and immunohistochemistry...
November 2003: Journal of Pediatric Surgery
https://www.readbyqxmd.com/read/11347467/-study-of-the-structural-and-structure-functional-subdomains-in-the-interphase-nucleus-by-photostabilization
#9
E V Sheval', A N Prusov, I I Kireev, V Iu Poliakov
The role of the nuclear matrix components in the organization of structural and functional domains of interphase nuclei was studied using irradiation with blue light in the presence of a photosensibilized agent (Ethidium bromide). Nuclear domain resistance to extractive solution (2 M NaCl) treatment served as a criterion of irradiation-induced stabilization of different nuclear domains. The following results have been obtained: 1) the structural organization of the complexes of chromatin and clusters of replication does not depend on the state of the nuclear matrix in isolated nuclei; 2) chemical stabilization of the nuclear matrix by Cu(2+)-ions is not sufficient for the organization of chromatin domains; 3) irradiation in the presence of Ethidium bromide stabilizes domains of the nuclei, but does not lead to stabilization of the nuclear matrix internal network...
2001: Tsitologiia
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