Promoting\nApoptosis in MCF‑7 Cells via ROS\nGeneration by Quinolino-triazoles Derived from One-Pot Telescopic\nSynthesis

Inhibition of vascular endothelial growth factor receptor\n2 (VEGFR-2)\nfacilitates potent antiangiogenic and anticancer responses. In this\nregard, the development of effective pharmacophores, i.e., quinoline-based\ntriazole derivatives <b>6a</b>–<b>j</b>, by a one-pot\ntelescopic approach is our focus. Among all of them, <b>6f</b>, possessing amide and cyanide substituents, displayed the highest\nbinding ability with VEGFR-2, having high affinity of −8.9\nkcal/mol. Further, <b>6f</b> and <b>6g</b> (containing\namide and bromo groups) exhibited a wide spectrum of anticancer activities\ndue to the presence of active oxidative stress inducers, with cytotoxicity\nvalues of 10 ± 0.2 and 12 ± 0.6 μM, respectively.\nApoptosis analysis demonstrated the involvement of <b>6f</b> and <b>6g</b> in mitochondrial damage and the loss of mitochondrial\nmembrane potential (ΔΨ<sub>m</sub>). Intercellular localization\nof <b>6f/6g</b> in MCF-7 revealed the presence of <b>6g</b> in the cytoplasm along with an increase in ROS production and a\nreduction in MMP, proving the ability of <b>6g</b> to target\nmitochondria.