1744-92-9Relevant academic research and scientific papers
NOVEL NUCLEIC ACID MODIFIERS
-
, (2019/07/20)
The present inventions generally relate to site-specific delivery of nucleic acid modifiers and includes novel DNA-binding proteins and effectors that can be rapidly programmed to make site-specific DNA modifications. The present inventions also provide a synthetic all-in-one genome editor (SAGE) systems comprising designer DNA sequence readers and a set of small molecules that induce double-strand breaks, enhance cellular permeability, inhibit NHEJ and activate HDR, as well as methods of using and delivering such systems.
Synthesis of novel heme-interacting acridone derivatives to prevent free heme-mediated protein oxidation and degradation
Pal, Chinmay,Kundu, Milan Kumar,Bandyopadhyay, Uday,Adhikari, Susanta
supporting information; experimental part, p. 3563 - 3567 (2011/08/06)
Heme is an important prosthetic molecule for various hemoproteins and serves important function in living aerobic organisms. But degradation of hemoprotein, for example, hemoglobin during different pathological conditions leads to the release of heme, which is very toxic as it induces oxidative stress and inflammation due to its pro-oxidant nature. Thus, synthesis of compound that will detoxify free heme by interacting with it would be fruitful for the management of heme-induced pathogenesis. Here, we report the synthesis of a novel natural product arborinine and some other acridone derivatives, which interact with free heme. These acridones in vitro block heme-mediated protein oxidation and degradation, markers for heme-induced oxidative stress.
Inhibition of Cryptosporidium parvum in vitro by 9-(alkylthio)acridine derivatives
Khalifa, Latifa,Rosales, Maria-Jose,Mascaro, Carmen,Karolak-Wojciechowska, Janina,Bsiri, Nadia,Brouant, Pierre,Barbe, Jacques
, p. 163 - 166 (2007/10/03)
The synthesis of several acridinic thioethers is described. Compounds prepared were tested in vitro as potential drugs against the opportunistic infection known as cryptosporidiosis. With a view to predict activity, the quantitative structure-activity relationships were investigated. Correlations between experimental data and either log P or pKa are discussed.
Structure-trypanodical activity relationships
Bsiri,Johnson,Kayirere,Galy,Galy,Barbe,Osuna,Mesa-Valle,Castilla Calvente,Rodriguez-Cabezas
, p. 27 - 33 (2007/10/03)
A set of 9-thioalkylacridinones, has been prepared and investigated' in vitro' against T. cruzi. Structure-antiparasitic activity relationships are detailed with a view to identify the major structural parameters for the activity under consideration.
Tricyclic heterocyclic derivatives
-
, (2008/06/13)
The invention relates to tricyclic heterocyclic derivatives, or pharmaceutically-acceptable salts or in vivohydrolysable esters thereof, which possess anti-cancer activity. The invention also relates to processes for the manufacture of said tricyclic hete
Substituent Effects on the Hydrolysis of Analogues of Nitracrine -1-nitroacridine>
O'Connor, Charmian J.,McLennan, Duncan J.,Denny, William A.,Sutton, Bridget M.
, p. 1637 - 1641 (2007/10/02)
Studies of the hydrolysis of the hypoxia-selective cytotoxic agent 9--1-nitroacridine (nitracrine) and several of its 4-substituted analogues and nitro-positional isomers have been carried out.Examination of the effects of pH and temperature on the hydrolysis of nitracrine itself shows that the reaction is subject to acid catalysis.The value of ΔH(excit.) increases from 46 to 63 kJ mol-1 as the pH falls from 6 to 3, while the value of ΔS(excit.) increases from -195 to -138 J k-1 mol-1.The rate constants for hydrolysis and the acid dissociation constants have been measured at pH 5 and 60 deg C.Both the rate constants of hydrolysis, corrected for the substrate-protonation equilibrium, and the substrate-acid association constants are well fitted by the Ehrenson-Brownlee-Taft dual-substituent-parameter ?R- relationship.The Swain-Unger-Rosenquist-Swain relationship shows weak correlation but the linear free-energy relationships of Hammett and Yukawa-Tsuno are not fitted.The results are discussed in terms of the resonance interactions of the possible intermediates in the hydrolysis pathways.
POLAROGRAPHIC INVESTIGATION OF THE KINETIC AND THERMODYNAMIC CHARACTERISTICS OF THE DEHALOGENATION OF SUBSTITUTED 6- AND 7-NITRO-9-CHLOROACRIDINES
Shapovalov, V. A.,Novotny, L.,Gaidukevich, A. N.,Bezuglyi, V. D.
, p. 2283 - 2285 (2007/10/02)
The kinetic relationships were obtained by the polarographic method and the thermodynamic parameters were calculated for the dehalogenation of 6- and 7-nitro-9-chloroacridines and indicate a two-stage process.It is suggested that an intermediate complex between the 9-chloroacridine and the corresponding acridone is formed in the reaction.
