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首页> 外文期刊>RSC Advances >Synthesis and biological evaluation of 3-amino-3-hydroxymethyloxindoles as potential anti-cancer agents
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Synthesis and biological evaluation of 3-amino-3-hydroxymethyloxindoles as potential anti-cancer agents

机译：3-氨基-3-羟基甲基羟吲哚类化合物作为潜在抗癌剂的合成及生物学评价

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A series of substituted 3-amino-3-hydroxymethyloxindoles (4a–4i) synthesized through a multi-component approach showed anticancer potency via in vitro cytotoxicity screening. Further, to develop the efficiency, derivatives (5a–5m) were synthesized and evaluated for their anti-proliferation activity. The most potent compound 5m showed cytotoxic effect toward SJSA-1 cells (IC50 = 3.14 μM) as well as inhibiting the growth of other cancer cell lines (HCT-116, Jurkat, KB and Bel7402). Further investigation revealed that 5m induced a significant G2/M cell cycle arrest and time- and dose-dependent cellular apoptosis in SJSA-1 cells. These results suggested that new compound 5m has anti-proliferating and pro-apoptotic effects, which might be a candidate for cancer therapies.
机译：通过多组分方法合成的一系列取代的3-氨基-3-羟基甲基羟吲哚（4a–4i）通过体外细胞毒性筛选显示了抗癌能力。此外，为了提高效率，合成了衍生物（5a-5m）并评估了它们的抗增殖活性。最有效的化合物5m对SJSA-1细胞（IC 50 = 3.14μM）具有细胞毒性作用，并抑制了其他癌细胞系（HCT-116， Jurkat，KB和Bel7402）。进一步的研究表明5m诱导了SJSA-1细胞中显着的G2 / M细胞周期停滞以及时间和剂量依赖性细胞凋亡。这些结果表明，新化合物5m具有抗增殖和促凋亡作用，这可能是癌症治疗的候选药物。

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