Therapeutic potential of Ag(i)-, Au(i)-, and Au(iii)-NHC complexes of 3-pyridyl wingtip N-heterocyclic carbenes (NHCs) against lung cancer

Herein, we report the easy synthetic approaches, structural features, theoretical studies, and extensive bioactivity of [Ag(1)(2)][PF6] (2), [Au(1)(2)][PF6] (3), and [Au(1)Cl-3] (4) compounds prepared from the NHC precursor 3-[(pyridin-3-yl)]imidazo[1,5-a]pyridin-4-ylium hexafluorophosphate (1HPF6). All the compounds were prepared and characterized by employing various spectroscopic techniques. The geometry of Au(I) complex, 3, was further confirmed using single-crystal X-ray diffraction (SCXRD) studies. DFT studies were performed to optimize the geometry and gain insights into the structure. The new compounds were implicated in studying their anti-oncogenic role in the most prevalent lung cancer. Anti-proliferative properties and very outstanding cytotoxicity were observed against various cancer cell lines but high potency towards lung cancer cells (A549) was observed. An MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide) assay of the drugs revealed their cytotoxicity and further study revealed that the drug plays a pivotal role in the mitochondrial reactive oxygen species (ROS)-dependent intrinsic apoptotic pathway. These studies widened the array of bioactive organometallics and revealed the remarkable efficacy of such compounds in solving therapeutic challenges.

Automated summary

This study reports the easy synthesis, structural features, theoretical studies, and extensive bioactivity of Ag and Au compounds prepared from a specific precursor. These compounds exhibit significant cytotoxicity against various cancer cells, particularly lung cancer cells (A549). Further research reveals that the compounds play a role in the mitochondrial reactive oxygen species (ROS)-dependent intrinsic apoptotic pathway.