Promoting Apoptosis in MCF-7 Cells via ROS Generation by Quinolino-triazoles Derived from One-Pot Telescopic
Joydip Mondal1, Tiasha Dasgupta2, Rakesh R Panicker1
1Department of Chemistry, School of Advanced Sciences, Vellore Institute of Technology (VIT), Vellore 632014, Tamil Nadu, India.
Abstract:
Inhibition of vascular endothelial growth factor receptor 2 (VEGFR-2) facilitates potent antiangiogenic and anticancer responses. In this regard, the development of effective pharmacophores, i.e., quinoline-based triazole derivatives 6a-j, by a one-pot telescopic approach is our focus. Among all of them, 6f, possessing amide and cyanide substituents, displayed the highest binding ability with VEGFR-2, having high affinity of -8.9 kcal/mol. Further, 6f and 6g (containing amide and bromo groups) exhibited a wide spectrum of anticancer activities due to the presence of active oxidative stress inducers, with cytotoxicity values of 10 ± 0.2 and 12 ± 0.6 μM, respectively. Apoptosis analysis demonstrated the involvement of 6f and 6g in mitochondrial damage and the loss of mitochondrial membrane potential (ΔΨm). Intercellular localization of 6f/6g in MCF-7 revealed the presence of 6g in the cytoplasm along with an increase in ROS production and a reduction in MMP, proving the ability of 6g to target mitochondria.
Related Concept Videos
Overview of Cell Death
Cell death was observed in the early 19th century, but there was no experimental evidence to prove it. In 1842, Carl Vogt first discovered cell death in a metamorphic toad; however, it was not termed ‘cell death.’ Scientists discovered different cell death pathways only in the...
Apoptosis
The Extrinsic Apoptotic Pathway
The Intrinsic Apoptotic Pathway
Phagocytosis of Apoptotic Cells
Normal cells contain receptors that prevent them from being recognized...
Cellular Injury V: Apoptosis and Autophagy


