Cytotoxic activity of proflavine diureas: synthesis, antitumor, evaluation and DNA binding properties of 1',1''-(acridin-3,6-diyl)-3',3''-dialkyldiureas.

Kozurkova M; Sabolova D; Janovec LMikes JKoval JUngvarsky JStefanisinova MFedorocko PKristian PImrich J

首页> 外文期刊>Bioorganic and medicinal chemistry >Cytotoxic activity of proflavine diureas: synthesis, antitumor, evaluation and DNA binding properties of 1',1''-(acridin-3,6-diyl)-3',3''-dialkyldiureas.

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Cytotoxic activity of proflavine diureas: synthesis, antitumor, evaluation and DNA binding properties of 1',1''-(acridin-3,6-diyl)-3',3''-dialkyldiureas.

机译：Cytotoxic activity of proflavine diureas: synthesis, antitumor, evaluation and DNA binding properties of 1',1''-(acridin-3,6-diyl)-3',3''-dialkyldiureas.

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The synthesis of novel 1',1''-(acridin-3,6-diyl)-3',3''-dialkyldiureas was reported. Their biological activity to inhibit cell proliferation was assessed by a MTT assay on two cell lines, HeLa and HCT-116, at micromolar concentration. 1',1''-(Acridin-3,6-diyl)-3',3''-dihexyldiurea hydrochloride was active on a HCT-116 cell line with an IC(50) value of 3.1 microM. The interaction of these compounds with calf thymus DNA was investigated by a variety of spectroscopic techniques including UV-vis, fluorescence and CD spectroscopy. From spectrofluorimetric titrations, binding constants for the DNA-drug complexes were determined (K=0.9-4.2x10(5) M(-1)). Antiproliferative activity of synthesized derivatives might be related to their intercalation into DNA.

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《Bioorganic and medicinal chemistry》 |2008年第7期|3976-3984|共9页
作者
Kozurkova M; Sabolova D; Janovec LMikes JKoval JUngvarsky JStefanisinova MFedorocko PKristian PImrich J;
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Department of Biochemistry, Institute of Chemistry, Faculty of Science, P. J. Safarik University, SK-04167 Kosice, Slovakia.;

ost.saga-med.ac.jp;

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正文语种英语
中图分类药学;生物化学;
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Acridines; Alkylation; Animals; Antineoplastic Agents; Apoptosis; Cattle; 吖啶类; 烷化作用; 动物; 抗肿瘤药; 脱噬作用; 牛; 分子结构; 光化学; 原黄素;

Cytotoxic activity of proflavine diureas: synthesis, antitumor, evaluation and DNA binding properties of 1',1''-(acridin-3,6-diyl)-3',3''-dialkyldiureas.

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