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首页> 外文期刊>Archives of Pharmacal Research >3-[(6-Arylamino)pyridazinylamino]benzoic acids: design, synthesis and in vitro evaluation of anticancer activity
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3-[(6-Arylamino)pyridazinylamino]benzoic acids: design, synthesis and in vitro evaluation of anticancer activity

机译:3-[(6-芳基氨基)哒嗪基氨基]苯甲酸:抗癌活性的设计,合成及体外评价

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摘要

A series of novel substituted 3,6-disubstituted pyridazines based on the structure of vatalanib (PTK787) were designed and synthesized. The cytotoxicity of the final compounds was tested in vitro on HT-29 colon cancer cell line. Compounds 2a and 2b with 4-chlorophenylamino moiety, exerted the highest cytotoxic activity with IC50 values equal to 15.3 and 3.9 μM respectively. The most promising compound, 2b, was found to be about fivefold more active than vatalanib against HT-29 colon cancer cell line.
机译:设计合成了一系列基于瓦他拉尼(PTK787)结构的新型3,6-二取代哒嗪。在HT-29结肠癌细胞系上体外测试了最终化合物的细胞毒性。具有4-氯苯基氨基部分的化合物2a和2b具有最高的细胞毒性活性,IC50值分别等于15.3和3.9μM。发现最有前途的化合物2b的抗HT-29结肠癌细胞系活性比瓦他拉尼高约五倍。

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