In the present study on the development of new anticonvulsants, 16 new1-(8-(benzyloxy)quinolin-2-yl-6-substituted-4,6-diazaspiro[2,4]heptane-5,7-diones were synthesized and tested for anticonvulsant activity using the maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ) screens, w...
Adiponectin is an adipocytokine with insulin-sensitizing, anti-atherogenic, and anti-inflammatory properties. Adiponectin secretion-inducing compounds have therapeutic potential in a variety of metabolic diseases. Phenotypic screening led to the discovery that 5,7-dihydroxy-8-(1-(4-hydroxy-3-met...
In this study, we investigated the effects of synthetic 6′-benzyloxy-4-bromo-2′-hydroxychalcone on viabilities of seven human leukaemia cells. It was cytotoxic against U-937, HL-60, K-562, NALM-6, MOLT-3 cells, and also against Bcl-2-overexpressing U-937/Bcl-2 cells and P-glycoprotein-overexpr...
A new radioiodination reagent, 3-iodophenylisothiocyanate (3-IPI) has been developed for coupling to monoclonal antibodies. The starting material, 3-tri-n-butylstannylphenylisothiocyanate was prepared via a reaction of hexabutylditin with 3-bromoaniline, followed by treatment with thiophosgene w...
N-Phenyl ureidobenzenesulfonates (PUB-SOs) are a new class of anticancer agents blocking the cell cycle progression in S-phase, inducing replicative stress and DNA double-strand breaks (DSBs). In this study, we evaluate the effect of modifying the nature and the position of different substituent...
Recently, several kinase inhibitors were found to also inhibit bromodomains, providing a new strategy for the discovery of bromodomain inhibitors. Along this line, starting from PLK1-BRD4 dual inhibitor BI-2536, we discovered a new series of dihydroquinoxalin-2(1H)-one with aniline and indoline ...
[email protected](Fe), with PdAu alloy nanoparticles of ca. 1.7 nm encapsulated inside MIL-100(Fe) cavities, were prepared via a double-solvent impregnation followed by photoreduction. As compared with bare [email protected](Fe), bimetallic [email protected](Fe) showed superior activities for th...
Reactions of 2-(diphenylphosphinomethyl)aniline, H2L1, with [MNCl2(PPh3)2] complexes (M = Re, Tc) give the bis-chelates [MNCl(H2L1)2]Cl (M = Re, Tc) or the mono-chelate [ReNCl2(PPh3)(H2L1)] depending on the conditions applied. The aminophosphine reacts as a bidentate, neutral ligand in all three...
Comparative studies on the image-wise formation of surface aniline moieties in monolayers of silica substrates prepared by the photodegradation of surface-adsorbed 4-aminophenyltrimethoxysilane and the photodeprotection of chemisorbed o-nitrobenzyl N-phenylcarbamate monolayers were described. Th...
A series of novel N-arylmethyl substituted piperidine-linked aniline derivatives were designed, synthesized and evaluated for their anti-HIV activity in MT-4 cells. All the new compounds showed moderate to potent activities against wild-type (wt) HIV-1 with an EC50 range from 0.022 to 2.1 μM. A...
Gold nanoparticles supported onto a nanoporous semicrystalline polymorphic polymer matrix consisting of syndiotactic polystyrene-cis-1,4-polybutadiene multiblock copolymer (AuNPs-sPSB) were investigated as catalyst in the reduction of nitroarenes into anilines using sodium borohydride as reducta...
Phosphoglycerate mutase 1 (PGAM1) coordinates glycolysis, pentose phosphate pathway, and serine synthesis to promote tumor growth through the regulation of its substrate 3-phosphoglycerate (3 PG) and product 2-phosphoglycerate (2 PG). Herein, based on our previously reported PGAM1 inhibitor PGMI...
25-azacycloartanol (1) is a potent inhibitor of S-adenosyl-L-methionine-cycloartenol-C-24-methyltransferase and of S-adenosyl-L-methionine-24-methylene lophenol-C-28-methyltransferase, two microsomal enzymes of maize (Zea mays) embryos. Addition of 1 to a suspension of bramble (Rubus fruticosus)...
The addition of 25-azacycloartanol to the medium of suspension cultures of bramble cells resulted, after 6 weeks of growth, in a large decrease in the percentage of C10 side-chain sterols, sitosterol and isofucosterol (83 % of the total in the control, 9 % in the treated cells), and in a spectac...
Poly(dialyldimethylammonium) (PDADMA) is a popular host for ion gel or composite polymer electrolytes for lithium batteries. Novel ternary systems are synthesised in this work by mixing high concentrations of lithium salt (lithium bis(fluorosulfonyl)imide (LiFSI)) with trimethylisobutylphosphoni...
Molten salts have attracted wide attention as electrolyte for lithium battery due to their nonvolatile and nonflammable features. In this work, the phase diagram of high pure lithium bis(fluorosulfonyl)imide (LiFSI) and KFSI binary system has been measured. This system shows a high transfer numb...
A new polymeric ionic liquid (PIL), poly(1-vinyl-3-methylimidazolium) bis(fluorosulfonyl)imide (PVyMIM-FSI), has been prepared by polymerization of the monomer of ionic liquids, 1-vinyl-3-methylimidazolium bis(fluorosulfonyl)imide (VyMIM-FSI). Its structure and composition have been characterize...
The binary eutectic mixture of lithium bis(fluorosulfonyl)imide (LiFSI) and potassium bis(fluorosulfonyl)imide (KFSI) with a molar ratio of xLiFSI: xKFSI = 0.41: 0.59 has been investigated as molten salt electrolyte for natural graphite/LiFePO4 lithium-ion cells at 80 °C. The electrochemical pe...
A novel electrolyte salt spiro-(1,1′)-bipyrrolidinium bis(fluorosulfonyl)imide (SBP-FSI) is successfully synthesized via one-step method in aqueous solvent. We systematically investigate, for the first time, physic-chemical properties and electrochemical stability of the new electrolyte. Compar...
Two new flavones, semiglabrinol and semiglabrin, have been isolated from Tephrosia semiglabra Sond. and their structures have been established as 2″′,2″′-dimethyl-3″′-hydroxy-tetrahydrofurano-[5″′, 4″′-b]-dihydrofurano[5″, 4″-h]flavone and the 3″′-O-acetate derivative, respectively...
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