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A One-Pot Three-Component Synthesis and Investigation of the In Vitro Mechanistic Anticancer Activity of Highly Functionalized Spirooxindole-Pyrrolidine Heterocyclic Hybrids

机译:高官能化螺氧吲哚 - 吡咯烷杂交物体外机械抗癌活性的单壶三组分合成及研究

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摘要

With an aim to develop more effective and affordable anticancer agents possessing a unique mechanism of action, we designed and synthesized derivatives of spirooxindole-pyrrolidine heterocyclic hybrids in good yields through a one-pot three-component (3+2) cycloaddition strategy. The synthesized compounds were characterized thoroughly for the physicochemical properties by making use of FT-IR, NMR spectroscopy, and mass spectrometry. Further, these compounds have been evaluated for the influence of anticancer activity against HepG2 cells up to 200 µg/mL concentration. The highly active molecular scaffold was tested for the in-depth mechanistic studies, and it was found that the major pathway of cell death is apoptosis which occurs through the induction of reactive oxygen species followed by the involvement of caspases.
机译:旨在开发更有效和价格实惠的抗癌剂,具有独特的作用机制,我们通过单罐三组分(3 + 2)环加入策略来设计和合成螺氧吲哚-吡咯烷杂交物的衍生物。通过使用FT-IR,NMR光谱和质谱法,将合成的化合物彻底用于物理化学性质。此外,已经评估了这些化合物的抗癌活性对高达200μg/ mL浓度的影响。测试高活性的分子支架进行了深入的机械研究,发现细胞死亡的主要途径是通过诱导反应性氧物种的凋亡,然后参与胱天蛋糖。

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