Herein we describe the synthesis of five new 2-aryl and 2-alkylimidazolone derivatives via an effective one-pot synthetic strategy assisted by microwave irradiations which allowed us to access the desired product in a reduced time reaction compared to the thermal heating and a slightly better yield (48% compared to 45%). The new imidazolone derivatives were evaluated for their anticancer activity in vitro against MCF-7, MDA-MB-231 and HepG2 cell lines. The results showed good cytotoxic effects for some of these derivatives on both MCF-7 and HepG2 cell lines in the range of 5.7–11.3 µM. Among the synthesized derivatives, 2ab and 2b showed the strongest activity with IC₅₀ values of 7 and 5.7 µM (MCF-7) and 6.2 and 8.6 µM (HepG2), respectively. The cytotoxic activities of these derivatives were moderate compared to those of doxorubicin. However, this product showed higher toxicity in vivo on the development of zebrafish embryos than the synthesized imidazolones. These derivatives at high concentrations exhibited some morphological abnormalities on the embryos.

在这里，我们描述了通过微波辐射辅助的有效一锅合成策略，通过一种有效的一锅合成策略合成了五个新的2-芳基和2-烷基咪唑啉酮衍生物，与热加热相比，这使我们能够在更短的时间内反应出所需的产物，并且反应稍好一些。收率（48％则为45％）。评价了新的咪唑啉酮衍生物在体外对MCF-7，MDA-MB-231和HepG2细胞系的抗癌活性。结果表明，这些衍生物中的一些在5.7-11.3 µM范围内对MCF-7和HepG2细胞系均具有良好的细胞毒性作用。在合成衍生物中，2ab和2b表现出最强的IC ₅₀活性值分别为7和5.7 µM（MCF-7）和6.2和8.6 µM（HepG2）。与阿霉素相比，这些衍生物的细胞毒活性中等。但是，该产品在体内对斑马鱼胚胎的发育显示出比合成的咪唑酮更高的毒性。这些高浓度的衍生物在胚胎上表现出一些形态异常。