22744-42-9Relevant academic research and scientific papers
Isouronium and N-hydroxyguanidinium derivatives as Cell growth inhibitors: A comparative study
Kahved?i?-Seljubac, Amila,Nathwani, Seema-Maria,Zisterer, Daniela M.,Rozas, Isabel
, p. 269 - 282 (2016)
Based on the results obtained from a computational study on the suitability of the isouronium and N-hydroxyguanidinium cations as hydrogen bond donors/acceptors, the DNA binding of a series of isouronium derivatives was assessed by DNA thermal denaturation experiments and compared to related N-hydroxyguanidines. Due to the poor DNA binding observed, the nature of the diaromatic linker was explored by preparing the corresponding amide-linked bis-isouronium derivative and measuring its DNA affinity. Next, the inhibitory effects of the isouronium derivatives on cell viability were evaluated in two different cancer cell lines providing IC50 values in the range of 36.9-57.4 μM (HL-60, leukemia), and 17.3-33.9 μM (Kelly, neuroblastoma). These values are comparable to those previously found for the N-hydroxyguanidine series. Compounds with the -S- linker (3, 6, and 10) proved to be considerably active in the HL-60 cells and even more active in the Kelly cell line. No correlation was found between DNA minor groove binding and cell growth inhibition; hence, activity may depend on different modes of action. Further studies into the apoptotic potential of these compounds indicated that, besides inhibiting cell viability and proliferation, derivatives 9 and 10, are significant apoptosis-inducers in both cell lines. Results obtained with HL-60 cells suggest that G2/M arrest and subsequent apoptosis induced by compound 10 are associated with microtubular depolymerisation, loss of mitochondrial membrane potential and activation of the caspase cascade. Moreover, the effects of compound 10 on cell viability and apoptosis in two non-cancereous cell lines (NIH3T3 and MCF-10A) indicate none or minimal toxicity.
ORGANIC COLORANT, COLORING COMPOSITION, AND INKJET INK
-
Paragraph 0098; 0099; 0100; 0101; 0102, (2019/01/25)
Organic colorant represented by General Formula (1) below: where in the General Formula (1), R1 and R2 each independently represent C1-C20 alkyl group, C1-C20 alkenyl group, phenyl group, naphthyl group, or group represented by —(CH
SuFEx-based synthesis of polysulfates
Dong, Jiajia,Sharpless, K. Barry,Kwisnek, Luke,Oakdale, James S.,Fokin, Valery V.
, p. 9466 - 9470 (2014/11/07)
High-molecular-weight polysulfates are readily formed from aromatic bis(silyl ethers) and bis(fluorosulfates) in the presence of a base catalyst. The reaction is fast and proceeds well under neat conditions or in solvents, such as dimethyl formamide or N-methylpyrrolidone, to provide the desired polymers in nearly quantitative yield. These polymers are more resistant to chemical degradation than their polycarbonate analogues and exhibit excellent mechanical, optical, and oxygen-barrier properties. High-molecular-weight polysulfates are readily formed from aromatic bis(silyl ethers) and bis(fluorosulfates) in the presence of a base catalyst. The polymers were obtained in nearly quantitative yield under neat conditions, they are more resistant to chemical degradation than their polycarbonate analogues and exhibit excellent mechanical, optical, and oxygen-barrier properties. BPA=bisphenol A.
N-Arylbenzamides: Extremely simple scaffolds for the development of novel estrogen receptor agonists
Caldarelli, Antonio,Minazzi, Paolo,Canonico, Pier Luigi,Genazzani, Armando A.,Giovenzana, Giovanni B.
, p. 148 - 152 (2013/04/23)
The research of estrogen receptor (ER) ligands has benefited in the last decade from the implementation of combinatorial chemistry. The general pharmacophore has been identified and subsequently a multitude of compounds have been synthesized. Surprisingly, up to now simple amides have not been taken into consideration. Here we show that amides resulting from the condensation of hydroxybenzoic acids with aminophenols result in compounds retaining the pharmacophore structure of an ER ligand with a clear estrogenic activity.
STILBENES AND CHALCONES FOR THE PREVENTION AND TREATMENT OF CARDIOVASCULAR DISEASES
-
Page/Page column 171, (2015/06/03)
The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis.
Diglycidyl ether of 4,4'-dihydroxy-α-methylstilbene
-
, (2008/06/13)
The diglycidyl ether of 4,4'-dihydroxy-α-methylstilbene is prepared.
Rodlike mesogenic thiirane resins (polythiiranes)
-
, (2008/06/13)
Polythiirane resins are disclosed which contain at least one, rodlike mesogenic moiety. These resins can be cured by conventional curing agents typically employed to cure epoxy resins or they can be thermally cured without a curing agent.
Mesogenic glycidyl esters
-
, (2008/06/13)
Glycidyl esters are disclosed which contain mesogenic moieties which result in improved properties when cured.
Syntheses and Reactions of (Trimethylsiloxy)benzoyl Chlorides
Schwarz, Gerd,Alberts, Heinrich,Kricheldorf, Hans R.
, p. 1257 - 1270 (2007/10/02)
The (trimethylsiloxy)benzoyl chlorides 1-7 are easily to obtain under mild conditions from silylated hydroxybenzoic acids by means of thionyl chloride.Whereas these acid chlorides are stable at room temperature, they undergo condensation polymerisation at temperatures above 100 deg C.Reactions with various nucleophils, such as thioalcohols, phenols, amines, N,O-bis(silylated)amino acids and N-silylated lactams were investigated.With hexamethyldisilazane and thionyl chloride the (trimethylsiloxy)benzonitriles 21, 22 are accessible, and by means of trimethylsilylazide the (trimethylsiloxy)phenyl isocyanates 23-25 were obtained.Conversion with phenyl carbazate and subsequent silylation lead to the 2-(trimethylsiloxy)phenyl-1,3,4-oxadiazol-5-ones 27a-c.
