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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, characterization and cytotoxicity of some novel 1,3-disubstituted-2,3-dihydro-2-iminobenzimidazoles.
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Synthesis, characterization and cytotoxicity of some novel 1,3-disubstituted-2,3-dihydro-2-iminobenzimidazoles.

机译：某些新型1,3-二取代-2,3-二氢-2-亚氨基苯并咪唑类化合物的合成，表征和细胞毒性。

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摘要

Some new 1,3-disubstituted-2,3-dihydro-2-iminobenzimidazoles were synthesized using 1-(un)substituted-2-aminobenzimidazoles as precursors in order to determine their cytotoxicity. The structures of the compounds were confirmed by IR, (1)H NMR, (13)C NMR and elemental analysis. Compounds 4, 7-11 and 13-14 were evaluated for their cytotoxical effect on two cancer cell lines: human colorectal cancer cell line HT-29, breast cancer cells MDA-MB-231 and as well as normal spleen cells. The distinctly marked antiproliferative activity of 1,3-bis(3-phenylpropyl-1)-1,3-dihydro-2H-benzimidazol-2-imine hydro bromide 7, N-(aminopropyl)-2-(3-{2-[(aminopropyl)-amino]-2-oxoethyl}-2-imino-2,3-dihydro-1H- benzimidazol-1-yl)acetamide 9 and 1,3-bis[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-2,3-dihydro-2H-benzimidazol-2-imin e 11 against human colorectal cancer cell line HT-29 was ascertained and the calculated IC(50) were 9.26, 0.56 and 0.013 nM respectively. Compounds 4, 9, 10 and 13 exhibited relative high cytotoxic activity against MDA-MB-231 cells. The calculated IC(50) values were in the range 0.123-1.65 nM. All tested compounds excluding compound 1,3-bis[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-2,3-dihydro-2H-benzimidazol-2-imin e (11) revealed proliferative activities to normal spleen cells. The computed EC(50) values varied from 0.05 to 16.91 nM.
机译：为了确定它们的细胞毒性，使用1-（未）取代的-2-氨基苯并咪唑作为前体合成了一些新的1，3-二取代的2，3-二氢-2-亚氨基苯并咪唑。通过IR，（1）H NMR，（13）C NMR和元素分析确认化合物的结构。评价化合物4、7-11和13-14对两种癌细胞系的细胞毒性作用：人结肠直肠癌细胞系HT-29，乳腺癌细胞MDA-MB-231以及正常脾细胞。 1,3-双（3-苯基丙基-1）-1,3-二氢-2H-苯并咪唑-2-亚胺氢溴酸盐7，N-（氨基丙基）-2-（3- {2- [（氨基丙基）-氨基] -2-氧乙基} -2-亚氨基-2,3-二氢-1H-苯并咪唑-1-基）乙酰胺9和1,3-双[2-（4-甲基哌嗪-1-基）确定）对人结肠直肠癌细胞系HT-29的）-2-氧代乙基] -2，3-二氢-2H-苯并咪唑-2-亚胺e 11，计算的IC（50）分别为9.26、0.56和0.013 nM。化合物4、9、10和13对MDA-MB-231细胞表现出相对较高的细胞毒活性。计算出的IC（50）值在0.123-1.65 nM的范围内。除化合物1,3-双[2-（4-甲基哌嗪-1-基）-2-氧代乙基] -2,3-二氢-2H-苯并咪唑-2-亚胺e（11）以外的所有测试化合物均显示出正常的增殖活性脾细胞。计算的EC（50）值从0.05到16.91 nM不等。

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