Imidazoacridinones arrest cell-cycle progression in the G2 phase of L1210 cells.


:Imidazoacridinones are a new class of highly potent antineoplastic agents synthesised at the Technical University of Gdansk. The pharmacophoric alkyldiamine group, which is also present in anthracenediones (e.g. ametantrone, mitoxantrone), has been shown to be responsible for their antineoplastic activity. In view of their chemical similarity to anthracenediones, we anticipated that the imidazoacridinones would have a mechanism of action similar to that of these agents and that this would be reflected by a similar influence on cell-cycle progression. Flow cytometry was used to monitor the effect of three derivatives of imidazoacridinone (C-1263, C-1310 and C-1311) on L1210 cell cycle traverse at concentrations ranging from 0.01 to 0.9 microgram/ml, corresponding to their 50% and 90% effective concentrations (EC50 and EC90 values), over times of drug treatment ranging from 1 to 48 h. The results demonstrate that all of the compounds produced a similar effect, inducing preferential and complete arrest (accumulation) of cells in the G2 phase of the cell cycle (i.e. G2 block). The kinetics of the induction of G2 arrest were dependent on both the dose and the duration of treatment. Cell-cycle arrest was reversible for up to about 3 h of treatment, being quite irreversible at longer incubation times. Microscopic inspection of cells performed in parallel with flow cytometry confirmed that imidazoacridinones induced a G2, not a G2/M, block.


Augustin E,Wheatley DN,Lamb J,Konopa J




Has Abstract


1996-01-01 00:00:00












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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章,评审


    authors: Bush H,Thatcher N,Barnard R

    更新日期:1979-01-01 00:00:00

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    更新日期:1989-01-01 00:00:00

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    更新日期:2020-05-01 00:00:00

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    authors: O'Dwyer PJ,King SA,Eisenhauer E,Grem JL,Hoth DF

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    journal_title:Cancer chemotherapy and pharmacology

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    journal_title:Cancer chemotherapy and pharmacology

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    journal_title:Cancer chemotherapy and pharmacology

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    journal_title:Cancer chemotherapy and pharmacology

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    authors: Sørensen PG,Nissen MH,Groth S,Rørth M

    更新日期:1985-01-01 00:00:00

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    pub_type: 杂志文章


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    pub_type: 临床试验,杂志文章,随机对照试验


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    更新日期:2015-06-01 00:00:00

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    journal_title:Cancer chemotherapy and pharmacology

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    authors: Izbicka E,Diaz A,Streeper R,Wick M,Campos D,Steffen R,Saunders M

    更新日期:2009-10-01 00:00:00

  • Comparison of leucovorin protection from variety of antifolates in human lymphoid cell lines.

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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章


    authors: Browman GP,Spiegl P,Booker L,Rosowsky A

    更新日期:1985-01-01 00:00:00

  • Modulation of adriamycin cytotoxicity and transport in drug-sensitive and multidrug-resistant Chinese hamster ovary cells by hyperthermia and cyclosporin A.

    abstract:PURPOSE:Chemosensitizers such as cyclosporin A can increase intracellular accumulation of chemotherapeutic agents such as Adriamycin in certain multidrug-resistant (MDR) cell lines with overexpression of P-glycoprotein. It is likely that, when combined with cyclosporin A, hyperthermia could increase membrane permeabili...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章


    authors: Larrivée B,Averill DA

    更新日期:2000-01-01 00:00:00

  • R-etodolac (SDX-101) and the related indole-pyran analogues SDX-308 and SDX-309 potentiate the antileukemic activity of standard cytotoxic agents in primary chronic lymphocytic leukaemia cells.

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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章


    authors: Lindhagen E,Nissle S,Leoni L,Elliott G,Chao Q,Larsson R,Aleskog A

    更新日期:2007-09-01 00:00:00