首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Design, synthesis and anticancer evaluation of novel tetrahydroquinoline derivatives containing sulfonamide moiety.
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Design, synthesis and anticancer evaluation of novel tetrahydroquinoline derivatives containing sulfonamide moiety.

机译:新型含磺酰胺部分的四氢喹啉衍生物的设计,合成和抗癌评估。

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摘要

Sulfonamides poses many types of biological activities and have recently been reported to show substantial antitumor activity in vitro and/or in vivo. There are a variety of mechanisms for the anticancer activity and the most prominent of these is through the inhibition of carbonic anhydrase isozymes. The present work reports the synthesis of some novel quinoline and pyrimido[4,5-b]quinoline derivatives bearing a substituted or unsubstituted sulfonamide moiety. The design of the structures of these compounds complies with the general pharmacophore of the sulfonamide compounds that act as carbonic anhydrase (CA) inhibitors as this may play a role in their anticancer activity. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against breast cancer cell line (MCF7). Most of the screened compounds showed interesting cytotoxic activities compared to a reference drug.
机译:磺酰胺具有许多类型的生物学活性,最近已报道其在体外和/或体内显示出显着的抗肿瘤活性。抗癌活性的机制多种多样,其中最突出的是抑制碳酸酐酶同工酶。本工作报告了一些新的喹啉和嘧啶并[4,5-b]喹啉衍生物的合成,这些衍生物带有取代或未取代的磺酰胺部分。这些化合物的结构设计符合充当碳酸酐酶(CA)抑制剂的磺酰胺化合物的一般药效,因为这可能在其抗癌活性中起作用。评价所有新合成的化合物对乳腺癌细胞系(MCF7)的体外抗癌活性。与参考药物相比,大多数筛选的化合物显示出令人感兴趣的细胞毒性活性。

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