The synthesis and antiproliferative effect of a novel curcumin analog, 4,4’-disulfonyldiarylidenyl piperidone, are reported. The design of the molecule is based on the fusion of an antiproliferative segment, namely diarylidenyl piperidone (DAP), with N-hyroxypyrroline, which is known to metabolically convert to nitroxide and protect healthy cells. Cellular uptake, metabolic conversion, cytotoxicity and antiproliferative effect of the DAP derivative against HCT-116 human colon cancer cells have been determined. Based on cell viability and proliferation assays as well as western-blot analysis of major transcription factors and inhibitory proteins, it is determined that the DAP compound is cytotoxic by inhibiting cell survival and proliferation pathways. The findings may have important implications in the design and development of effective anticancer agents.

中文翻译：

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新型4,4'-二磺酰基二芳基哌啶酮在人结肠癌细胞中的抗增殖作用。

报道了新型姜黄素类似物4,4'-二磺酰基二芳基烯基哌啶酮的合成和抗增殖作用。分子的设计基于抗增殖段即二芳基哌啶酮（DAP）与N的融合-羟吡咯啉，已知可代谢转化为氮氧化物并保护健康细胞。已经确定了DAP衍生物对HCT-116人结肠癌细胞的细胞摄取，代谢转化，细胞毒性和抗增殖作用。基于细胞活力和增殖测定以及主要转录因子和抑制蛋白的蛋白质印迹分析，可以确定DAP化合物通过抑制细胞存活和增殖途径而具有细胞毒性。这些发现可能对有效抗癌药的设计和开发具有重要意义。