- Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents
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The design, synthesis, biophysical and biochemical evaluation is presented of a new series of benzylamino-substituted acridines as G-quadruplex binding telomerase inhibitors. Replacement of the previously reported anilino substituents by benzylamino group
- Martins, Cristina,Gunaratnam, Mekala,Stuart, John,Makwana, Vaidahi,Greciano, Olga,Reszka, Anthony P.,Kelland, Lloyd R.,Neidle, Stephen
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- Fluorinated 3,6,9-trisubstituted acridine derivatives as DNA interacting agents and topoisomerase inhibitors with A549 antiproliferative activity
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A series of new 3,6,9-trisubstituted acridine derivatives with fluorine substituents on phenyl ring were synthesized and their interaction with calf thymus DNA was investigated. Analysis using UV–Vis absorbance spectra provided valuable information about
- Nunhart, Patrik,Konko?ová, Eva,Janovec, Ladislav,Jend?elovsky, Rastislav,Vargová, Jana,?evc, Juraj,Matejová, Mária,Miltáková, Beata,Fedoro?ko, Peter,Kozurkova, Mária
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Read Online
- Antiprotozoal activity and DNA binding of dicationic acridones
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Dicationic acridone derivatives were synthesized and their antiparasitic activity was evaluated. Acridones displayed in vitro nanomolar IC50 values against Trypanosoma brucei rhodesiense STIB900 with selectivity indices >1000. Compounds 1b, 3a,
- Montalvo-Quirós, Sandra,Taladriz-Sender, Andrea,Kaiser, Marcel,Dardonville, Christophe
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supporting information
p. 1940 - 1949
(2015/04/21)
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- CANCER TREATMENT USING SPECIFIC 3,6,9-SUBSTITUTED ACRIDINES
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The present invention relates to a 3,6,9 acridine compound and optionally substituted derivatives thereof that may be useful in the treatment of cancer. The invention also provides compositions comprising the compounds and uses thereof.
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- Therapeutic acridone and acridine compounds
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The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ═O, L is —H, alpha is a single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is
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Page/Page column 36; sheet 1
(2008/06/13)
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- The proton transfer reaction between bis(2,4-dinitrophenyl)methane and nitrogen bases in dimethyl sulfoxide and toluene solvents
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Rate constants have been measured for the proton and deuteron transfer reactions of bis(2,4-dinitrophenyl)methane (1) with 1,1,3,3-tetramethylguanidine (TMG) and 1,5-diazabicycloundec-7-ene (DBU) in dimethyl sulfoxide (DMSO) and toluene solvents.Eq
- Jarczewski, Arnold,Schroeder, Grzegorz,Leffek, Kenneth T.
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p. 468 - 473
(2007/10/02)
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- Transient nitronic acid formation in the protonation of the carbanion of 2,2',4,4'-tetranitrodiphenylmethane in acidic methanol
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Rates of deprotonation of 2.2',4,4'-tetranitrodiphenylmethane (1) by a variety of bases B- and of protonation of the resulting carbanion (2) by the conjugated acids BH in methanol have been measured at 20 deg C.The Broensted αBH coefficients for protonation of 2 by phenol and carboxylic acid buffers are equal to 0.58 and 0.43 respectively, as compared with αBH values of 0.59 and 0.52 respectively, for the same reactions in 50percent H2O-50percent DMSO.On the other hand, a comparison of the intrinsic rate constants kBH0 (in the Marcus sense) in the two solvents reveals that the effect of going from 50percent H2O - 50percent DMSO to methanol is is to lower kArOH0 for the phenol reactions by a factor 2 but to increase kRCOOH0 for carboxylic acid reactions by a factor of 5.It is shown that the solvent effects on αBH and kBH0 can all be understood in the context of the Principle of Imperfect Synchronisation (PIS) recently proposed by Bernasconi.In addition, a fast equilibrium protonation of the carbanion 2 is found to precede its conversion to 1 at low pH, i.e., pHa value associated with the ionization of 2,H is ca 4.25
- Terrier, Francois,Lelievre, Jacques,Chatrousse, Alain-Pierre,Schaal, Robert,Farrell, Patrick, G.
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p. 1980 - 1986
(2007/10/02)
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- Solvent Dependence of the Ionization of Nitrophenylmethanes
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The solvent dependence of proton abstraction from various nitrophenylmethanes has been examined for aqueous dimethyl sulphoxide and methanolic dimethyl sulphoxide solutions.Even though the compounds studied vary considerably in thermodynamic acidity (pKa), their proton-abstraction rates all show the same solvent dependence.It is suggested that the transition states for these reactions all occur at similar positions on the reaction pathway, and that transition state imbalances exist for these proton transfers.
- Fogel, Paula,Farrel, Patrick G.,Lelievre, Jacques,Chatrousse, Alain P.,Terrier, Francois
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p. 711 - 716
(2007/10/02)
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