首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and in vitro anticancer screening of some novel 4-(2-amino-3-cyano-4-substituted-5,6,7,8-tetrahydroquinolin-1-(4H)-yl)benzenesulf onamides.
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Synthesis and in vitro anticancer screening of some novel 4-(2-amino-3-cyano-4-substituted-5,6,7,8-tetrahydroquinolin-1-(4H)-yl)benzenesulf onamides.

机译:一些新型的4-(2-氨基-3-氰基-4-取代的5,6,7,8-四氢喹啉-1-(4H)-基)苯磺酰胺的合成及体外抗癌筛选。

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摘要

It has been reported that aryl/heteroaryl sulfonamide compounds may act as anticancer agents through a variety of mechanisms and the most prominent of these mechanisms is through the inhibition of carbonic anhydrase isozymes. The present work reports the possible utility of 4-(cyclohexenylamino)benzenesulfonamide in the synthesis of some novel 4-(quinolin-1-yl)benzenesulfonamide derivatives 6a-u. The structures of these compounds were confirmed by elemental analyses, IR, (1)H NMR and mass spectral data. All the newly synthesized compounds were evaluated for their in vitro anticancer activity. Some compounds showed interesting in vitro anticancer activities when compared with doxorubicin as a reference drug. In addition, docking of the synthesized compounds into carbonic anhydrase isozyme II (CA II) active site was performed in order to give a suggestion about the proposed mechanism of action.
机译:据报道,芳基/杂芳基磺酰胺化合物可通过多种机制充当抗癌剂,并且这些机制中最突出的是通过抑制碳酸酐酶同工酶。本工作报道了4-(环己烯基氨基)苯磺酰胺在某些新型的4-(喹啉-1-基)苯磺酰胺衍生物6a-u的合成中的可能用途。这些化合物的结构通过元素分析,IR,(1)H NMR和质谱数据证实。评价所有新合成的化合物的体外抗癌活性。与阿霉素作为参考药物相比,某些化合物具有令人感兴趣的体外抗癌活性。另外,进行合成化合物对接至碳酸酐酶同工酶II(CA II)活性位点,以便对所提出的作用机理提出建议。

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