Indium (III) thiosemicarbazone 5b is an anticancer agent.1 It is cytotoxic to A549, MCF-7 breast, MCF-7/DDP cisplatin-resistant breast, and Hl 7702 liver cancer cells (IC50s = 2.41, 1.97, 2.11, and 8.95 µM, respectively). Indium (III) thiosemicarbazone 5b decreases PI3K, Akt, mTOR, P-gp, and GSH levels in MCF-7/DDP cells. In vivo, indium (III) thiosemicarbazone 5b (2.5 µmol/kg) reduces tumor weight and volume in an MCF-7/DDP mouse xenograft model. Liposomes containing indium (III) thiosemicarbazone 5b also induce apoptosis and pro-death autophagy in MCF-7/DDP cells, as well as reduce tumor volume and weight in an MCF-7/DDP mouse xenograft model.
1.Jiang, M., Chu, Y., Yang, T., et al.Developing a novel indium(III) agent based on liposomes to overcome cisplatin-induced resistance in breast cancer by multitargeting the tumor microenvironment componentsJ. Med. Chem.64(19)14587-14602(2021)