Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, Wuhan, China.
Chem Biol Drug Des. 2017 Apr;89(4):634-638. doi: 10.1111/cbdd.12884. Epub 2016 Nov 19.
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.
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。