3-Methoxy-Pyrrole-based small molecule damages mitochondria to instigate apoptosis in breast cancer cells

Abstract

Mitochondrion has been implicated in the development and progression of breast cancer, making it an unconventional target for the anti-cancer therapy. As a result, there is a need to explore novel small molecules for next generation breast cancer therapy. Towards this endeavour, herein, we have identified a novel 3-methoxy-pyrrole-based small molecule from a synthetic library. Confocal fluorescence microscopy studies revealed that, this lead small molecule induced mitochondrial damage and generated reactive oxygen species (ROS) in the MCF7 breast cancer cells. Small molecule based mitochondrial impairment subsequently triggered cell cycle arrest and nuclear DNA damage followed by apoptosis leading remarkable cell killing and inhibition in the colony formation in MCF7 cells. Moreover, this 3-methoxy-pyrrole killed drug resistant MDA-MB-231 triple negative breast cancer cells and OVCAR8 ovarian cancer cells efficiently. This novel small molecule can open a new direction towards mitochondria targeted breast cancer therapy in future.