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Rhodium(III)–Picolinamide Complexes Act as Anticancer and Antimetastasis Agents via Inducing Apoptosis and Autophagy

Yun‐Qiong Gu, Kun Yang, Qi‐Yuan Yang, Huanqing Li, Mei‐Qi Hu, Meng‐Xue Ma, Nan-Feng Chen, Yang-Han Liu, Hong Liang, Zhen‐Feng Chen

2023Journal of Medicinal Chemistry34 citationsDOI

Abstract

As a continuation of our endeavors in discovering metal-based drugs with cytotoxic and antimetastatic activities, herein, we reported the syntheses of 11 new rhodium(III)–picolinamide complexes and the exploration of their potential anticancer activities. These Rh(III) complexes showed high antiproliferative activity against the tested cancer cell lines in vitro. The mechanism study indicated that Rh1 ([Rh( 3a )(CH 3 CN)Cl 2 ]) and Rh2 ([Rh( 3b )(CH 3 CN)Cl 2 ]) inhibited cell proliferation by multiple modes of action via cell cycle arrest, apoptosis, and autophagy and inhibited cell metastasis via FAK-regulated integrin β1-mediated suppression of EGFR expression. Furthermore, Rh1 and Rh2 significantly inhibited bladder cancer growth and breast cancer metastasis in a xenograft model. These rhodium(III) complexes could be developed as potential anticancer agents with antitumor growth and antimetastasis activity.

Topics & Concepts

ChemistryAutophagyApoptosisCytotoxic T cellMetastasisIn vitroCancer researchCell growthRhodiumCancer cellCell cycle checkpointMechanism of actionCytotoxicityGrowth inhibitionCell biologyCell cycleCancerBiochemistryBiologyGeneticsCatalysisMetal complexes synthesis and propertiesClick Chemistry and ApplicationsFerrocene Chemistry and Applications
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