- Synthesis of noncyclic carriers for cerium ion transport through polymer inclusion membrane
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Noncyclic ionophores having both diphenylphosphinyl methylcarbamoyl and N,N-di(2-ethylhexyl)carbamoylmethoxy groups were synthesized for cerium ion transport through polymer inclusion membrane. The derivative of 3-aminopropanol having these groups was fou
- Hiratani, Kazuhisa,Kusumocahyo, Samuel Puriyantoro,Kameta, Naohiro,Sugaya, Kenta,Shinbo, Toshio,Kanamori, Toshiyuki
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- Bimodal ligands with macrocyclic and acyclic binding moieties, complexes and compositions thereof, and methods of using
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Substituted 1,4,7-triazacyclononane-N,N′,N″-triacetic acid and 1,4,7,10-tetraazacyclcododecane-N,N′,N″,N′″-tetraacetic acid compounds with a pendant amino or hydroxyl group, metal complexes thereof, compositions thereof, and methods of making and use in diagnostic imaging and treatment of cellular disorders.
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Page/Page column 73
(2015/09/23)
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- Bimodal ligands with macrocyclic and acyclic binding moieties, complexes and compositions thereof, and methods of using
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Substituted 1,4,7-triazacyclononane-N,N′,N″-triacetic acid and 1,4,7,10-tetraazacyclcododecane-N,N′,N″,N′″-tetraacetic acid compounds with a pendant amino or hydroxyl group, metal complexes thereof, compositions thereof, and methods of making and use in diagnostic imaging and treatment of cellular disorders.
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- Synthesis and evaluation of novel polyaminocarboxylate-based antitumor agents
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Iron depletion, using iron chelators targeting transferrin receptor (TfR) and ribonucleotide reductase (RR), is proven to be effective in the treatment of cancer. We synthesized and evaluated novel polyaminocarboxylate-based chelators NETA, NE3TA, and NE3TA-Bn and their bifunctional versions C-NETA, C-NE3TA, and N-NE3TA for use in iron depletion tumor therapy. The cytotoxic activities of the novel polyaminocarboxylates were evaluated in the HeLa and HT29 colon cancer cell lines and compared to the clinically available iron depletion agent DFO and the frequently explored polyaminocarboxylate DTPA. All new chelators except C-NETA displayed enhanced cytotoxicities in both HeLa and HT29 cancer cells compared to DFO and DTPA. Incorporation of the nitro functional unit for conjugation to a targeting moiety into the two potent non-functionalized chelators NE3TA and NE3TA-Bn (C-NE3TA and N-NE3TA) was well-tolerated and resulted in a minimal decrease in cytotoxicity. Cellular uptake of C-NE3TA, examined using a confocal microscope, indicates that the chelator is taken up into HT29 cancer cells.
- Chong, Hyun-Soon,Ma, Xiang,Lee, Haisung,Bui, Phuong,Song, Hyun A.,Birch, Noah
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p. 2208 - 2215
(2008/12/21)
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- N-Nitrosation of (E)-2-(benzylidene-amino)ethanols
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Reaction of (E)-2-(benzylidene-amino)ethanol 2 with nitric oxide afforded an (E)-rotamer dominant mixture of (E)- and (Z)-N-nitroso-2-aryl-1,3-oxazolidine 3 at room temperature in good overall yields.
- Peng, Li-jun,Liu, Zhong-quan,Wang, Jian-tao,Wu, Long-min
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p. 7418 - 7421
(2008/03/13)
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- Ugi multicomponent reaction followed by an intramolecular nucleophilic substitution: Convergent multicomponent synthesis of 1-sulfonyl 1,4-diazepan-5-ones and of their benzo-fused derivatives
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A short, two-step approach to the synthesis of diazepane or diazocane systems, based on a Ugi multicomponent reaction followed by a subsequent intramolecular SN2 reaction was studied. 1 -Sulfonyl tetrahydrobenzo[e]-1,4-diazepin-1-ones 1 were ob
- Banfi, Luca,Basso, Andrea,Guanti, Giuseppe,Kielland, Nicola,Repetto, Claudio,Riva, Renata
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p. 2151 - 2160
(2007/10/03)
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- Oxidation of secondary amines catalyzed by dirhodium caprolactamate
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The dirhodium caprolactamate [Rh2(cap)4] catalyzed oxidation of secondary amines to imines by tert-butyl hydroperoxide (TBHP) occurs with high chemo- and regioselectivity. The Royal Society of Chemistry.
- Choi, Hojae,Doyle, Michael P.
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p. 745 - 747
(2007/10/03)
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- Asymmetric synthesis of 3-hydroxy-pyrrolidines via tin-lithium exchange and cyclization
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We report a method for the synthesis of chiral pyrrolidines using tin-lithium exchange and cyclization reactions. The precursors are formed readily from simple starting materials and undergo tin-lithium exchange by treatment with n-butyllithium. Subsequent intramolecular carbolithiation is stereoselective to give highly enantiomerically enriched pyrrolidines in excellent yields.
- Christoph, Guido,Stratmann, Christian,Coldham, Iain,Hoppe, Dieter
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p. 4469 - 4471
(2007/10/03)
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- Multicomponent synthesis of dihydrobenzoxazepinones by coupling Ugi and Mitsunobu reactions
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Various dihydrobenzo[f][1,4]oxazepin-5-ones have been convergently prepared in 2-3 steps by coupling Ugi and Mitsunobu reactions. Two alternative methodologies were used: in the first one the Ugi condensation was followed by a Mitsunobu cyclization (2 ste
- Banfi, Luca,Guanti, Giuseppe,Basso, Andrea,Lecinska, Paulina,Riva, Renata
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p. 4236 - 4240
(2008/09/18)
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- o-Iodoxybenzoic Acid (IBX) as a Viable Reagent in the Manipulation of Nitrogen- and Sulfur-Containing Substrates: Scope, Generality, and Mechanism of IBX-Mediated Amine Oxidations and Dithiane Deprotections
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o-Iodoxybenzoic acid (IBX), a highly versatile hypervalent iodine(V) reagent, was found to efficiently mediate the dehydrogenation of amines in addition to facilitating the oxidative cleavage of dithioacetals and dithioketals. Through the development of relevant IBX-based protocols, a plethora of useful synthetic intermediates, including imines, oximes, ketones, and aromatic N-heterocycles, were found to be readily accessible under notably mild conditions. Further investigation of these transformations led to the elucidation of valuable mechanistic details, resulting in the conclusion that they proceed via ionic rather than single electron transfer (SET) pathways.
- Nicolaou,Mathison, Casey J. N.,Montagnon, Tamsyn
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p. 5192 - 5201
(2007/10/03)
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- New reactions of IBX: Oxidation of nitrogen- and sulfur-containing substrates to afford useful synthetic intermediates
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New reactions for the synthetic toolbox: 2-lodoxybenzoic acid (IBX) was employed to access a diverse array of useful synthetic intermediates. Among other transformations, the developed chemistry converts amines into imines, dithianes into carbonyl groups, N-heterocycles into N-heteroaromatic compounds, and hydroxylamines into oximes in high yields.
- Nicolaou,Mathison, Casey J. N.,Montagnon, Tamsyn
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p. 4077 - 4082
(2007/10/03)
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- Oxazolidine and thiazolidine derived carbodithioate compositions useful as vulcanization accelerators
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Oxazolidine and thiazolidinecarbodithioates, and pyridine adducts thereof, are accelerators for the vulcanization of EPDM elastomers, wherein they exhibit non-blooming characteristics.
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