- Evaluation of biological properties of 3,3′,4,4′-benzophenonetetracarboxylic dianhydride derivatives and their ability to inhibit hexokinase activity
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This investigation has explored the properties of 3,3′,4,4′-benzophenonetetracarboxylic dianhydride (BDTA) derivatives with regard to their being prospective inhibitors of hexokinase II (HKII). A pluripotent embryonic carcinoma cell line P19 (ECC), was used as the biological target for newly generated potential inhibitors of HKII. The results obtained from Virtual High-Throughput Screening (VHTS), molecular modeling and biological activity studies showed BDTA to be a promising leading structure with a good binding score and simplest functionalization. The inhibitory effect was measured after 72?h incubation. Of selected BDTA derivatives, the most active was compound 3b, containing 3-hydroxyphenyl moiety in the para position, being able at 100?μM to decrease the mass of differentiated P19dCs cells by 30%, changing both the mitochondrial transmembrane potential and reactive oxygen species level. Under these conditions, only compound 3b had the ability to decrease hexokinase activity in a dose-dependent manner.
- Kochel, Krzysztof,Tomczyk, Mateusz D.,Sim?es, Rui F.,Fr?czek, Tomasz,Soboń, Adrian,Oliveira, Paulo J.,Walczak, Krzysztof Z.,Koceva-Chy?a, Aneta
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- Microwave-assisted synthesis and characterization of optically active poly (ester-imide)s incorporating l-alanine
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Pyromellitic dianhydride (1) was reacted with L-alanine (2) to result [N,N'-(pyromellitoyl)-bis-l-alanine diacid] (3). This compound (3) was converted to N,N'-(pyromellitoyl)-bis-l-alanine diacyl chloride (4) by reaction with thionyl chloride. The microwave-assisted polycondensation of this diacyl chloride (4) with polyethyleneglycol-diol (PEG-200) and/or three synthetic aromatic diols furnish a series of new PEIs and Co-PEIs in a laboratory microwave oven (Milestone). The resulting polymers and copolymers have inherent viscosities in the range of 0.31-0.53 dl g-1. These polymers are optically active, thermally stable and soluble in polar aprotic solvents such as DMF, DMSO, NMP, DMAc, and sulfuric acid. All of the above polymers were fully characterized by IR spectroscopy, 1H NMR spectroscopy, elemental analyses, specific rotation and thermal analyses. Some structural characterizations and physical properties of these optically active PEIs and Co-PEIs have been reported.
- Zahmatkesh, Saeed,Hajipour, Abdol R.
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experimental part
p. 1253 - 1260
(2010/08/06)
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- New copoly(ether-imide-sulfone) oligomers having pendant ionic groups
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New copoly(ether-imide-sulfone) oligomers have been synthesized by solution polycondensation reaction of bis(pchlorophenyl)sulfone with various imide bisphenols and 2,2-bis(4-hydroxyphenyl)-propane (Bisphenol A). The Williamson polyetherification procedur
- Ciobanu, Manuela,Brunchi, Cristina-Eliza,Perju, Elena,Cozan, Vasile,Bruma, Maria
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experimental part
p. 685 - 692
(2010/07/02)
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