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Jaroslaw Dziegielewski et al.
Biochemical pharmacology, 63(9), 1653-1662 (2002-05-15)
Imidazoacridinones (IA) are a class of antitumor agents which includes C-1311, an interesting drug in clinical trials. This study investigated the mechanism of IA binding to DNA for a series of 13 analogs that differ in their cytotoxic potency. Using
Magdalena Hyzy et al.
Biochemical pharmacology, 69(5), 801-809 (2005-02-16)
In this study, we investigated the cell death process induced by imidazoacridone C-1311 (Symadex) in HT-29 human colon carcinoma cells which have been shown to be preferentially sensitive to this compound in experimental tumour models both in vitro and in
Zofia Mazerska
Acta biochimica Polonica, 50(2), 515-525 (2003-07-02)
The present work is part of a wide research project aimed to elucidate the mechanism of the metabolic activation of the antitumor imidazoacridinone agent C-1311 selected for clinical trials. The objectives of the investigations presented here were: (i) to examine
Agnieszka Potega et al.
Drug metabolism and disposition: the biological fate of chemicals, 39(8), 1423-1432 (2011-05-11)
5-Diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) is an antitumor agent that is also active against autoimmune diseases. The intention of the present studies was to elucidate the role of selected liver enzymes in metabolism of C-1311 and the less active 8-methyl derivative, 5-diethylaminoethylamino-8-methoxyimidazoacridinone (C-1330).
Zofia Mazerska et al.
Biochemical pharmacology, 66(9), 1727-1736 (2003-10-18)
The imidazoacridinone derivative, C-1311, is an antitumor agent that has been under phase I of clinical trial. The work presented here aims to elucidate the molecular mechanism of the enzymatic oxidative activation of this drug in such a model metabolic
Jolanta Paradziej-Łukowicz et al.
Cancer biology & therapy, 12(7), 586-597 (2011-07-22)
Antitumor imidazoacridinone C-1311 is a DNA-reactive topoisomerase II and FLT3 receptor tyrosine kinase inhibitor. Here, we demonstrate the mechanism of C-1311 inhibitory action on novel targets: hypoxia-inducible factor-1α (HIF-1α), vascular-endothelial growth factor (VEGF), and angiogenesis. In a cell-free system, C-1311
Cinzia De Marco et al.
International journal of oncology, 31(4), 907-913 (2007-09-06)
The cytotoxic activity of the imidazoacridinone C1311 was related to its effect on cell cycle progression in 16 human cell lines from different solid tumour types and leukaemias. A 72-h exposure to C1311 induced a wide range of growth inhibition
Marie Suggitt et al.
International journal of oncology, 29(6), 1493-1499 (2006-11-08)
We describe a modified hollow fibre assay (HFA) for investigating the potential of novel molecules as pharmaceutical agents. In particular the assay provides drug/target interaction data that can facilitate the selection of lead compounds for further evaluation in more sophisticated
Anna Skwarska et al.
Apoptosis : an international journal on programmed cell death, 12(12), 2245-2257 (2007-10-10)
Imidazoacridinone C-1311 is a DNA-targeting antitumor intercalator/alkylator currently undergoing Phase II clinical trials. Here, we elucidated the sequence of death responses to C-1311 in human leukemia MOLT4 cells using drug concentration (30 nM) that causes near complete cell growth inhibition
Monique W J den Brok et al.
Journal of pharmaceutical and biomedical analysis, 39(1-2), 46-53 (2005-05-19)
C1311 (5-[[2-(diethylamino)ethyl]amino]-8-hydroxyimidazo [4,5,1-de]-acridin-6-one-dihydrochloride trihydrate) is the lead compound from the group of imidazoacridinones, a novel group of rationally designed anticancer agents. The pharmaceutical development of C1311 necessitated the availability of an assay for the quantification and purity determination of C1311
Monique W J den Brok et al.
Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, 11(1), 13-19 (2006-02-08)
C1311 is the lead compound from the imidazoacridinones, a novel group of rationally designed anti-cancer agents. The compound is pharmaceutically formulated as a lyophilized product containing 100 mg C1311 (anhydrous free base) per dosage unit and requires reconstitution before intravenous
Agata Kowalczyk et al.
Analytical and bioanalytical chemistry, 392(3), 463-469 (2008-08-22)
A piece of dry N-isopropylacrylamide polymer was soaked in phosphate buffer to obtain a hydrogel which was then employed in the examination of interactions between an anticancer drug C-1311 (5-diethylaminoethyl-amino-8-hydroxyimidazoacridinone) and dsDNA. dsDNA was introduced into the polymer at the
Ewelina Zabost et al.
Physical chemistry chemical physics : PCCP, 14(10), 3408-3413 (2012-02-03)
Several medicinally important compounds that bind to dsDNA strands via intercalation (C-1311, C-1305, EtBr), major groove binding (Hoechst 33258) and covalent binding (cis-Pt) were examined. The obtained results suggest that both the transfer of conformation B to C and the
Barbara Fedejko-Kap et al.
Drug metabolism and disposition: the biological fate of chemicals, 40(9), 1736-1743 (2012-06-05)
5-Diethylaminoethylamino-8-hydroxyimidazoacridinone, C-1311 (NSC-645809), is an antitumor agent shown to be effective against breast cancer in phase II clinical trials. A similar compound, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, shows high activity against experimental tumors and is expected to have even more beneficial pharmacological properties
Anna M Nowicka et al.
Analytical and bioanalytical chemistry, 389(6), 1931-1940 (2007-10-18)
A method is presented for the electroanalytical characterization of interactions of dsDNA with a drug, under conditions that both agents are dissolved in the phosphate buffer solution and both are electroactive. Normal pulse, square wave, differential pulse, and cyclic voltammetries
Monika Pawlowska et al.
Drug metabolism and disposition: the biological fate of chemicals, 41(2), 414-421 (2012-11-20)
The acridinone derivates 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) and 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) are promising antitumor agents with high activity against several experimental cellular and tumor models and are under evaluation in preclinical and early phase clinical trials. Recent evidence from our laboratories has indicated
Eran E Bram et al.
Biochemical pharmacology, 74(1), 41-53 (2007-05-08)
The A421 ABCG2 genotype is a frequent polymorphism encoding the K141 transporter, which is associated with a significant decrease in transporter expression and function when compared to the wild type (wt) C421 allele encoding the Q141 ABCG2. Here we show
Monique W J Den Brok et al.
PDA journal of pharmaceutical science and technology, 59(5), 285-297 (2005-12-01)
C1311 (5-[[2-(diethylamino)ethyl]amino]-8-hydroxyimidazo [4,5,1-de]-acridin-6-one-dihydrochloride trihydrate) is the lead compound from the group of imidazoacridinones, a novel group of rationally designed anticancer agents. C1311 shows significant cytotoxic activity in vitro and in vivo toward a range of colon tumours. The aim of
Barbara Fedejko-Kap et al.
Xenobiotica; the fate of foreign compounds in biological systems, 41(12), 1044-1055 (2011-08-24)
5-Dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, being the close structural analogue of the clinically tested imidazoacridinone anti-tumour agent, C-1311, expressed high activity against experimental tumours and is expected to have more advantageous pharmacological properties than C-1311. The aim of this study was to elucidate
Joanna Polewska et al.
The Journal of pharmacology and experimental therapeutics, 346(3), 393-405 (2013-07-05)
Imidazoacridinone 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) is an antitumor inhibitor of topoisomerase II and FMS-like tyrosine kinase 3 receptor. In this study, we describe the unique sequence of cellular responses to C-1311 in human non-small cell lung cancer (NSCLC) cell lines, A549 and
Anna Skwarska et al.
Oncotarget, 8(19), 31187-31198 (2017-04-19)
C-1311 is a small molecule, which has shown promise in a number of pre-clinical and clinical studies. However, the biological response to C-1311 exposure is complicated and has been reported to involve a number of cell fates. Here, we investigated
Anita Wiśniewska et al.
Acta biochimica Polonica, 54(4), 831-838 (2007-12-18)
The imidazoacridinone derivative C-1311 is an antitumor agent in Phase II clinical trials. The molecular mechanism of enzymatic oxidation of this compound in a peroxidase model system was reported earlier. The present studies were performed to elucidate the role of
N Alami et al.
Journal of chemotherapy (Florence, Italy), 19(5), 546-553 (2007-12-13)
The aim of this study was to investigate the antiproliferative effects of C-1311 (Symadex), a member of the imidazoacridinone family, in human colorectal cancer cells. In the in vitro screen, C-1311 led to the most prominent growth inhibition in HT29
V V S Rajendra Prasad et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 43(4), 217-224 (2011-05-14)
A series of novel N(10)-substituted acridone derivatives bearing alkyl side-chain with tertiary amine groups at the terminal position were evaluated for their in vitro cytotoxic effects against drug sensitive and resistant cancer cell lines. All the molecules were designed on
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