Preparation and Bioactivity of Iridium(III) Phenanthroline Complexes with Halide Ions and Pyridine Leaving Groups |
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| Authors: | Dr Xicheng Liu Mingxiao Shao Congcong Liang Jinghang Guo Guangxuan Wang Xiang-Ai Yuan Zhihong Jing Laijin Tian Prof?Dr Zhe Liu |
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| Affiliation: | Institute of Anticancer Agents Development and Theranostic Application, The Key Laboratory of Life-Organic Analysis and Key Laboratory of Phar maceutical Intermediates and, Analysis of Natural Medicine, School of Chemistry and Chemical Engineering, Qufu Normal University, Jining Shi, Qufu, 273165 P. R. China |
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| Abstract: | A series of half-sandwich structural iridium(III) phenanthroline (Phen) complexes with halide ions (Cl?, Br?, I?) and pyridine leaving groups ((η5-CpX)Ir(Phen)Z](PF6)n, Cpx: electron-rich cyclopentadienyl group, Z: leaving group) have been prepared. Target complexes, especially the Cpxbiph (biphenyl-substituted cyclopentadienyl)-based one, showed favourable anticancer activity against human lung cancer (A549) cells; the best one ( Ir8 ) was almost five times that of cisplatin under the same conditions. Compared with complexes involving halide ion leaving groups, the pyridine-based one did not display hydrolysis but effectively caused lysosomal damage, leading to accumulation in the cytosol, inducing an increase in the level of intracellular reactive oxygen species and apoptosis; this indicated an anticancer mechanism of oxidation. Additionally, these complexes could bind to serum albumin through a static quenching mechanism. The data highlight the potential value of half-sandwich iridium(III) phenanthroline complexes as anticancer drugs. |
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| Keywords: | anticancer agents hydrolysis iridium(III) complexes leaving groups |
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