66074-67-7Relevant academic research and scientific papers
Synthesis, cytotoxicity and structure-activity relationships between ester and amide functionalities in novel acridine-based platinum(II) complexes
Bouyer, Florence,Moretto, Johnny,Pertuit, David,Szollosi, Anna,Lacaille-Dubois, Marie-Aleth,Blache, Yves,Chauffert, Bruno,Desbois, Nicolas
, p. 51 - 57 (2012)
In order to improve the pharmacological profile of the anticancer drug cisplatin, several new acridine-based tethered (ethane-1,2-diamine)platinum(II) complexes connected by a polymethylene chain were synthetized. Activity-structure relationship between amide or ester functionalities was explored by changing acridine-9-carboxamide into acridine-9-carboxylate chromophore. The in vitro cytotoxicity of these new complexes was assessed in human colic HCT 116, SW480 and HT-29 cancer cell lines. Series of complexes bearing the acridine-9-carboxylate chromophore displayed higher cytotoxic effect than acridine-9-carboxamide complexes, with gradual effect according to the size of the polymethylene linker.
A nitroxyl synthase catalytic antibody
Bahr, Nicolaus,Güller, Rolf,Reymond, Jean-Louis,Lerner, Richard A.
, p. 3550 - 3555 (1996)
An antibody raised against acridinium hapten 1 is shown to catalyze the retro Diels-Alder reaction of the anthracene-HNO cycloadduct 2 to release anthracene 4 and nitroxyl (HNO). Nitroxyl is oxidized to nitric oxide (NO) in the presence of superoxide dism
Study of a potential inhibitor of acetylcholinesterase using UV spectrophotometry, NMR spectroscopy and molecular modeling
Correia, Isabelle,Ronzani, Nello,Platzer, Nicole,Doan, Bich-Thuy,Beloeil, Jean-Claude
, p. 148 - 156 (2006)
1-[6-(Acridine-9-carbonyloxy)hexyl]pyridinium chloride (1) was synthesized and studied as a potential inhibitor of acetylcholinesterase (AChE), which is frequently involved in Alzheimer's disease. UV spectrophotometry showed that 1 is a reversible and competitive inhibitor of AChE (Ki ≈ 2 × 10-7 M). NMR (TrNOESY) showed that 1, bonded to AChE, maintains an extended form that allows hydrophobic interactions to occur between the aliphatic chain and the deep and narrow gorge of AchE and favors interactions between the acridine group and the catalytic and anionic subsites situated at the bottom of the gorge, and also between the pyridinium ring and the peripheral site. A more detailed picture of the structure of the complex was obtained by combining NMR structural data and molecular modeling (docking, dynamics simulation and energy calculations). Copyright
Synthesis and characterization of polyamine-based biomimetic catalysts as artificial ribonuclease
Shinozuka,Nakashima,Shimizu,Sawai
, p. 117 - 130 (2001)
Several polyamine derivatives (I-V) conjugated with or without an intercalative moiety were prepared as ribonuclease mimics. Although no DNA-cleaving activity was observed for all compounds tested, mimics I, III, and V bearing an intercalative moiety alon
Synthesis and antimicrobial activity of acridine carboxylic acid derivatives containing a piperazine moiety
Kudryavtseva,Lamanov, A. Yu.,Klimova,Nazarov
, p. 123 - 128 (2017)
A convenient method for the synthesis of new acridine derivatives containing a piperazine moiety was developed. Antimicrobial activity against some pathogenic microorganisms was established for a series of the synthesized compounds.
Metal complexes of modified cyclen as catalysts for hydrolytic restriction of plasmid DNA
Krauser, Joel A.,Joshi, Aarti L.,Kady, Ismail O.
, p. 877 - 884 (2010)
Simple and novel nuclease models have been synthesized. These involve metal-binding ligand 1,4,7,10-tetraazlcyclododecane (cyclen) tethered to an acridine ring (a DNA-binding group) by amide linkers of various lengths. Binding of these probes to DNA was s
9-(2,6-Difluorophenoxycarbonyl)-10-methylacridinium trifluoromethane- sulfonate and its precursor 2,6-difluorophenyl acridine-9-carboxylate: C-H...O, C-F...π, S-O...π and π-π stacking interactions
Sikorski, Artur,Krzyminski, Karol,Niziolek, Agnieszka,Blazejowski, Jerzy
, p. o690-o694 (2005)
The title compounds, C21H14F2NO 2+·CF3SO3-, (I), and C20H11F2NO2, (II), form monoclinic and triclinic crystals, respectivel
A Novel Multifunctionally Labelled DNA Probe Bearing an Intercalator and a Fluorophore
Shinozuka, Kazuo,Seto, Yoshiaki,Sawai, Hiroaki
, p. 1377 - 1378 (1994)
A 15-mer DNA labelled with a novel multifunctional fluorescent agent bearing acridine and fluorescein moieties is synthesized and the intensity of fluorescein-based fluorescence detected by the excitation of acridine is shown to be strongly affected by the DNA's secondary structure.
DINUCLEATING LIGAND OR DINUCLEAR METAL COMPLEX
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Paragraph 0112-0113, (2021/03/19)
To provide a dinuclear metal complex that can be synthesized simply and easily and has a proper anticancer action.SOLUTION: The present disclosure provides a dinucleating ligand represented by the following formula (I) and a dinuclear metal complex thereof (where each X may be the same or different to represent H, Cl, OMe, or, Me, Y is H, a phenyl group, a substituted carbamoyl group or the like).SELECTED DRAWING: None
AMINE OR (THIO)AMIDE CONTAINING LXR MODULATORS
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Page/Page column 81, (2019/02/06)
The present invention relates to derivatives of formula (I) which bind to the liver X receptor (LXRα and/or LXRβ) and act preferably as inverse agonists of LXR.
