- Synthesis, photophysical and electrochemical properties of stilbenoid dendrimers with phenothiazine surface group
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Synthesis of some novel stilbenoid dendrimers with the phenothiazine surface group has been achieved using Horner-Wadsworth-Emmons (HWE) and click reactions through convergent methodology. Alkyl chains have been incorporated at the periphery of phenothiaz
- Satheeshkumar, Chinnadurai,Ravivarma, Mahalingam,Rajakumar, Perumal,Ashokkumar, Rajamani,Jeong, Dong-Cheol,Song, Changsik
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- Nanomolar inhibitors of the transcription factor STAT5b with high selectivity over STAT5a
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Src homology 2 (SH2) domains play a central role in signal transduction. Although many SH2 domains have been validated as drug targets, their structural similarity makes development of specific inhibitors difficult. The cancer-relevant transcription facto
- Elumalai, Nagarajan,Berg, Angela,Natarajan, Kalaiselvi,Scharow, Andrej,Berg, Thorsten
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supporting information
p. 4758 - 4763
(2015/04/14)
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- ω-haloalkylphosphoryl compounds: Synthesis and properties
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A general method of the synthesis of ω-haloalkylphosphoryl compounds was developed, a series of compounds of phosphonic and phosphine oxide type were synthesized. The ability of some ω-haloalkylphosphonates to undergo intramolecular cyclization into the corresponding 1,2-oxaphospholane and 1,2-oxaphosphorine was investigated depending on the solvent polarity, the presence of halogen ions in the solution, and temperature. Tetrahydrofuran was chosen as one of the most suitable solvents for the alkylation of CH acids with ω-haloalkylphosphoryl compounds.
- Ragulin
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p. 1928 - 1937
(2013/06/05)
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- Phenolic bis-styrylbenzenes as β-amyloid binding ligands and free radical scavengers
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Starting from bisphenolic bis-styrylbenzene DF-9 (4), β-amyloid (Aβ) binding affinity and specificity for phenolic bis-styrylbenzenes, monostyrylbenzenes, and alkyne controls were determined by fluorescence titration with β-amyloid peptide Aβ1-40 and a fluorescence assay using APP/PS1 transgenic mouse brain sections. Bis-styrylbenzene SAR is derived largely from work on symmetrical compounds. This study is the first to describe Aβ binding data for bis-styrylbenzenes unsymmetrical in the outer rings. With one exception, binding affinity and specificity were decreased by adding and/or changing the substitution pattern of phenol functional groups, changing the orientation about the central phenyl ring, replacing the alkene with alkyne bonds, or eliminating the central phenyl ring. The only compound with an Aβ binding affinity and specificity comparable to 4 was its 3-hydroxy regioisomer 8. Like 4, 8 crossed the blood-brain barrier and bound to Aβ plaques in vivo. By use of a DPPH assay, phenol functional groups with para orientations seem to be a necessary, but insufficient, criterion for good free radical scavenging properties in these compounds.
- Flaherty, Daniel P.,Kiyota, Tomomi,Dong, Yuxiang,Ikezu, Tsuneya,Vennerstrom, Jonathan L.
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supporting information; experimental part
p. 7992 - 7999
(2011/03/19)
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- Synthesis of rigid π-conjugated mono-, bis-, tris-, and tetrakis(terpyridine)s: Influence of the degree and pattern of substitution on the photophysical Properties
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A series of rigid π-conjugated mono-, bis-, tris-, and tetrakis-(terpyridine)s 3-8 was synthesized in high yields by means of Horner-Wadsworth-Emmons (HWE) reactions between benzyl phosphonates 1 and an aldehyde-functionalized ter-pyridine derivative 2. The photophysical properties of the materials in solution and in the solid state depend strongly both on the numbers of terpyridine moieties attached to the central phenyl cores and on the geometries of the compounds. The photophysical behavior of the ortho-substituted compounds 5 and 8 indicated significant changes in the geometries, together with major extensions of the effective π-conjugated systems upon excitation. Bright green emission with high quantum yields was observed for the tetrakis(ter-pyridine) derivative 8.
- Winter, Andreas,Friebe, Christian,Hager, Martin D.,Schubert, Ulrich S.
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supporting information; experimental part
p. 801 - 809
(2009/07/05)
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- Use of benzylphosphonic acid derivatives for the treatment of diseases caused by viruses
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The use of a compound of the formula I STR1 in which V is an alkyl group, fluorine, chlorine, bromine, or iodine, n is an integer from 1 to 5, W is an alkyl, alkenyl, alkynyl or alkoxy group, cyanide, nitro, carboxyl, hydrogen or a cycloalkyl, aryl, aralkyl or carboalkoxy group, R1 and R2 are an alkyl, alkenyl, alkynyl, cycloalkyl or halogenoalkyl group, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium, triethylammonium or hydrogen, R1 and R2 together form a cyclic diester, R3 and R4 are an alkyl, alkenyl, alkynyl, carboalkoxy, cycloalkyl or alkoxy group, hydrogen, fluorine, chlorine, bromine or iodine and X, Y and Z are oxygen or sulfur, for the treatment of diseases caused by DNA viruses or RNA viruses is described.
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