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合成新型芳基异恶唑-氧吲哚共轭物作为有效的增殖抑制剂。

Synthesis of new arylisoxazole-oxindole conjugates as potent antiproliferative agents.

机构信息

Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, Wuhan, China.

出版信息

Chem Biol Drug Des. 2017 Apr;89(4):634-638. doi: 10.1111/cbdd.12884. Epub 2016 Nov 19.

Abstract

A new series of arylisoxazole-oxindole derivatives (6a-r) were synthesized and evaluated for their antiproliferative activity against human cancer cell lines including non-small cell lung (A549), cervical (HeLa), breast (MCF-7), and prostate (DU-145) cancer cell lines. The synthesized compounds (6a-r) demonstrated excellent to moderate cytotoxicity with IC values ranging from 0.82 to 3.69 μm. Some new compounds (6m-r) exhibited profound cytotoxicity better or similar to positive control. More particularly, the compound 6q possesses donating substituent like methoxy group presented at 5-position on D ring exhibited remarkable antiproliferative activity against A-549 (lung cancer) with an IC value 0.82 μm. Further studies to determine the mechanistic aspects of these conjugates are under progress.

摘要

我们合成了一系列新型芳基异噁唑-氧吲哚衍生物(6a-r),并评估了它们对人癌细胞系(包括非小细胞肺癌(A549)、宫颈(HeLa)、乳腺癌(MCF-7)和前列腺癌(DU-145))的抗增殖活性。合成的化合物(6a-r)表现出优异到中等的细胞毒性,IC 值范围为 0.82-3.69μm。一些新的化合物(6m-r)表现出明显的细胞毒性,优于或类似于阳性对照。特别是,化合物 6q 具有供电子取代基,如在 D 环的 5 位上的甲氧基,对 A-549(肺癌)表现出显著的抗增殖活性,IC 值为 0.82μm。目前正在进行进一步的研究,以确定这些化合物的作用机制。

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