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Synthesis of 2-aryl-4-(benzimidazol-2-yl)-1,2-dihydro[1,2,4]triazino-[4,5-a]benzimidazol-1-one derivatives with preferential cytotoxicity against carcinoma cell lines
J Styskala, L Styskalova, J Slouka, M Hajduch
Language English Country France
- MeSH
- Benzimidazoles pharmacology chemical synthesis chemistry toxicity MeSH
- Financing, Organized MeSH
- Humans MeSH
- Cell Line, Tumor MeSH
- Cell Proliferation drug effects MeSH
- Antineoplastic Agents pharmacology chemical synthesis chemistry toxicity MeSH
- Drug Design MeSH
- Sensitivity and Specificity MeSH
- Check Tag
- Humans MeSH
In this paper we describe the preparation of some derivatives of 1,2,4-triazino[4,5-a]benzimidazol-1-ones (5 and 6), containing additional benzimidazole ring. These compounds were prepared using coupling reactions of diazonium salts with 1,1-bis(1-ethoxycarbonyl-benzimidazol-2-yl)methane (2) to obtain unstable hydrazones 4, which readily undergo cyclization. Interestingly, the selected compounds demonstrated preferential cytotoxic activities against human carcinoma and glioma cell lines compared with leukemic cells. They showed significant activity against multidrug-resistant P-glycoprotein expressing cell lines but had less effect on multidrug-resistance protein 1 positive and topoisomerase IIalpha negative leukemias.
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- $a Stýskala, Jakub, $d 1972- $7 ola2005284375
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- $a Synthesis of 2-aryl-4-(benzimidazol-2-yl)-1,2-dihydro[1,2,4]triazino-[4,5-a]benzimidazol-1-one derivatives with preferential cytotoxicity against carcinoma cell lines / $c J Styskala, L Styskalova, J Slouka, M Hajduch
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- $a Department of Organic Chemistry, Faculty of Science, Palacky University, Tr. Svobody 8, 771 46 Olomouc, Czech Republic.
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- $a In this paper we describe the preparation of some derivatives of 1,2,4-triazino[4,5-a]benzimidazol-1-ones (5 and 6), containing additional benzimidazole ring. These compounds were prepared using coupling reactions of diazonium salts with 1,1-bis(1-ethoxycarbonyl-benzimidazol-2-yl)methane (2) to obtain unstable hydrazones 4, which readily undergo cyclization. Interestingly, the selected compounds demonstrated preferential cytotoxic activities against human carcinoma and glioma cell lines compared with leukemic cells. They showed significant activity against multidrug-resistant P-glycoprotein expressing cell lines but had less effect on multidrug-resistance protein 1 positive and topoisomerase IIalpha negative leukemias.
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- $a Slouka, Jan, $d 1935- $7 jn20000402233
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- $a Hajdúch, Marián, $d 1969- $7 xx0050218
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- $t European Journal of Medicinal Chemistry $w MED00001628 $g Roč. 43, č. 3 (2008), s. 449-455 $x 0223-5234
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