首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and cytotoxicity evaluation of 1-(3-(9H-carbazol-4-yloxy)-2-hydroxypropyl)-3-aryl-1H-pyrazole-5-carboxylic acid derivatives.
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Synthesis and cytotoxicity evaluation of 1-(3-(9H-carbazol-4-yloxy)-2-hydroxypropyl)-3-aryl-1H-pyrazole-5-carboxylic acid derivatives.

机译:合成和细胞毒性评价1-(3-(9H-咔唑-4-基氧基)-2-羟丙基)-3-芳基-1H-吡唑-5-羧酸衍生物。

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摘要

Several novel molecules, 1-(3'-(9H-carbazol-4-yloxy)-2'-hydroxypropyl)-3-aryl-1H-pyrazole-5-carboxylic acid derivatives 3a-g were synthesized and screened to evaluate their cytotoxicity against cancer cells in vitro. The compounds 3a-g has been prepared by the reaction of ethyl 3-aryl-1H-pyrazole-5-carboxylate with 4-oxiranylmethoxy-9H-carbazole in moderate to excellent yields. The cytotoxicity of synthesized compounds was evaluated by a SRB (sulforhodamine B) assay against cancer cell such as SK-N-SH human neuroblastoma (NB), human A549 lung carcinoma, human breast cancer MCF-7 cell lines. The results showed that seven compounds can suppress SK-N-SH tumor cancer cell growth. Among them, compound 3d was the most effective small molecule in inhibiting SK-N-SH cell growth.
机译:合成并筛选合成几种新的分子1-(3' - (3' - (9H-咔唑-4-基氧基)-2'-羟丙基)-3-芳基-1H-吡唑-5-羧酸衍生物3a-g以评估它们的细胞毒性 对抗体外癌细胞。 通过将3-芳基-1H-吡唑-5-羧酸甲酸乙酯与4-氧基丙基甲氧基-9H-咔唑的反应中等至优异的产率来制备化合物3a-g。 通过SRB(荧光酚胺B)测定法评估合成化合物的细胞毒性,例如SK-N-SH人神经母细胞瘤(NB),人A549肺癌,人乳腺癌MCF-7细胞系。 结果表明,七种化合物可以抑制SK-N-Sh肿瘤癌细胞生长。 其中,复合3D是抑制SK-N-SH细胞生长的最有效的小分子。

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