- Synthesis of a bifunctional boron-Lewis acid and studies on host-guest chemistry using pyridine and TMPD
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Based on the previously described bifunctional Lewis acid with a functional distance of the boron functions of 4.918(2) ?, the development of a further bifunctional, boron-containing Lewis acid with a wider functional distance is demonstrated. Again, a st
- Mitzel, Norbert W.,Neumann, Beate,Rudlof, Jens,Stammler, Hans-Georg
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- Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A
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A series of symmetric molecules incorporating aryl or pyridyl moieties as central core and 1,4-substituted triazoles as a side bridge was synthesised. The new compounds were investigated as lactate dehydro-genase (LDH, EC 1.1.1.27) inhibitors. The cancer associated LDHA isoform was inhibited with IC50 = 117–174?μM. Seven compounds exhibited better LDHA inhibition (IC50 117–136?μM) compared to known LDH inhibitor–galloflavin (IC50 157?μM).
- Altamimi, Abdul-Malek S.,Abdel-Gawad, Sherif A.,Alafeefy, Ahmed M.,Balode, Agnese,Vozny, Igor,Pustenko, Aleksandrs,?alubovskis, Raivis,El Shikh, Mohey Eldin,Alasmary, Fatmah A. S.
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p. 147 - 150
(2018/01/02)
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- Control of supramolecular nanoassemblies by tuning the interactions of bent-shaped rod-coil molecules
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Rod-coil molecules 1a, 1b and 2a, 2b, consisting of biphenyl and phenyl units connected by an acetylene bond as the rod segment and oligo(ethylene glycol) (OEG) as the coil segment, were synthesized and characterized. Molecules 1a and 1b incorporate a but
- You, Shengnan,Zhong, Keli,Jin, Long Yi
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p. 3334 - 3340
(2017/07/10)
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- Synthesis of chiral 1,3-bis(1-(diarylphosphoryl)ethyl)-benzenes via Ir-catalyzed double asymmetric hydrogenation of bis(diarylvinylphosphine oxides)
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A class of chiral 1,3-bis(diarylphosphinoethyl)benzenes, which are key intermediates for the synthesis of PCP-type chiral pincer ligands, were prepared in high diastereomeric ratios and excellent ee values via double asymmetric hydrogenation of the corresponding bis(diarylvinylphosphine oxide) substrates using a SpinPhox/Ir(I) complex as the catalyst. The hydrogenation product 5a was readily transformed into the corresponding borane-protected chiral PCP-type pincer ligand 7a with high enantiomeric excess, exemplifying a viable synthetic route to optically active chiral PCP pincer ligands.
- Liu, Xu,Han, Zhaobin,Wang, Zheng,Ding, Kuiling
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p. 1073 - 1078
(2014/08/18)
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- Aerobic oxynitration of alkynes with tBuONO and TEMPO
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An efficient method for stereoselective nitroaminoxylation of alkyne has been reported. The reaction enjoys a broad substrate scope, good functional group tolerance, and high yields. Synthetically useful α-nitroketones can be accessed through these products in a single step.
- Dutta, Uttam,Maity, Soham,Kancherla, Rajesh,Maiti, Debabrata
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supporting information
p. 6302 - 6305
(2015/02/19)
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- Expedient synthesis of SMAMPs via click chemistry
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A novel series of synthetic mimics of antimicrobial peptides (SMAMPs) containing triazole linkers were assembled using click chemistry. While only moderately active in buffer alone, an increase in antimicrobial activity against Staphylococcus aureus and Escherichia coli was observed when these SMAMPs were administered in the presence of mouse serum. One compound had minimum inhibitory concentrations (MICs) of 0.39 μg/mL and 6.25 μg/mL, respectively, and an HC50 of 693 μg/mL. These values compared favorably to peptide-based antimicrobials. A correlation between the net positive charge and SMAMP antimicrobial activity was observed. The triazole linker, an amide surrogate, was found to provide better antimicrobial activity against both S. aureus and E. coli when compared to other analogues.
- Fu, Tsung-Hao,Li, Yan,Thaker, Hitesh D.,Scott, Richard W.,Tew, Gregory N.
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supporting information
p. 841 - 845
(2013/10/01)
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- Synthesis and biological evaluation of new bis-indolone-N-oxides
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A series of bis-indolone-N-oxides, 1a-f, was prepared from bis(ethynyl)benzenes and o-halonitroaryls and studied for their in vitro antiplasmodial activities against Plasmodium falciparum and representative strains of bacteria and candida as well as for their cytotoxicity against a human tumor cell line (MCF7). They did not cause any haemolysis (300 μg mL-1). Of the synthesized bis-indolones, compound 1a had the most potent antiplasmodial activity (IC50 = 0.763 μmol L-1 on the FcB1 strain) with a selectivity index (CC50 MCF7/IC 50 FcB1) of 35.6. No potency against the tested microbial strains was observed.
- Najahi, Ennaji,Valentin, Alexis,Tene, Nathan,Treilhou, Michel,Nepveu, Francoise
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- Ph(O) group for protection of terminal acetylenes
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A protecting group Ph(O) for terminal ethyne was newly developed. This protecting group can be introduced readily to terminal ethyne by CuI-catalyzed phosphination and subsequent oxidation with H Ph(O)-protected ethynes remained intact in Sonogashira coup
- Yang, Xin,Matsuo, Daisuke,Suzuma, Yoshinori,Fang, Jing-Kun,Xu, Feng,Orita, Akihiro,Otera, Junzo,Kajiyama, Shingo,Koumura, Nagatoshi,Hara, Kohjiro
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supporting information; experimental part
p. 2402 - 2406
(2011/11/05)
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- Intramolecular hydrogen bonds preorganize an aryl-triazole receptor into a crescent for chloride binding
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Figure presented Aryl-triazole pentads have been preorganized with intramolecular hydrogen bonds to enhance chloride binding. This outcome highlights the dual hydrogen bond donor and acceptor properties of 1,2,3-triazoles.
- Lee, Semin,Hua, Yuran,Park, Hyunsoo,Flood, Amar H.
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supporting information; experimental part
p. 2100 - 2102
(2010/06/20)
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- Counting the monomers in nanometer-sized oligomers by pulsed electron-electron double resonance
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In a lot of cases active biomolecules are complexes of higher order, thus methods capable of counting the number of building blocks and elucidating their geometric arrangement are needed. Therefore, we experimentally validate here spin-counting via 4-puls
- Bode, Bela E.,Margraf, Dominik,Plackmeyer, Joern,Duerner, Gerd,Prisner, Thomas F.,Schiemann, Olav
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p. 6736 - 6745
(2008/02/09)
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- Meta-conjugation and excited-state coupling in phenylacetylene dendrimers
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Traditional pictures of optical properties in phenylacetylene dendrimers view the molecule as a collection of independent chromophores, linked by meta-substitution at the central phenyl ring. While this picture is reasonable for explaining the observed ab
- Gaab, Kevin M.,Thompson, Alexis L.,Xu, Jianjun,Martinez, Todd J.,Bardeen, Christopher J.
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p. 9288 - 9289
(2007/10/03)
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- Synthesis of High Carbon Materials from Acetylenic Precursors. Preparation of Aromatic Monomers Bearing Multiple Ethynyl Groups
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The synthesis of polyethynyl aromatics as starting materials for the preparation of highly cross-linked organic solids containing high atom fractions of carbon is described.Treatment of bromo- and iodoaromatic compounds with (trimethylsilyl)acetylene (TMSA) in the presence of palladium(O) and copper(I) in amine solvents yields (trimethylsilyl)ethynyl-substituted aromatics.The TMS protecting groups can be removed by hydrolysis with mild base.Compounds prepared by using this technique include 1,3-diethynylbenzene, 2,5-diethynylthiophene, 1,3-diethynyltetrafluorobenzene, 1,4-diethynyltetrafluorobenzene, 2-ethynylthiazole, 2,4-diethynylthiazole, 2,7-diethynylnaphthalene, hexakis((trimethylsilyl)ethynyl)benzene, tetraethynylthiophene, 2,5-bis((trimethylsilyl)ethynyl)-3,4-bis(3-hydroxy-3-methyl-1-butynyl)thiophene, 2,5-diethynyl-3,4-bis(3-hydroxy-3-methyl-1-butynyl)thiophene, 2,5-bis(4-(2-thienyl)butadiynyl)-3,4-bis(3-hydroxy-3-methyl-1-butynyl)thiophene, and 2,5-bis-(4-(2-thienyl)butadiynyl)-3,4-diethynylthiophene.
- Neenan, Thomas X.,Whitesides, George M.
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p. 2489 - 2496
(2007/10/02)
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