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Synthesis and Antitumor Activity Evaluation of Cyclometalated 2H-Indazole Ruthenium(II) and Iridium(III) Complexes.
ChemPlusChem ( IF 3.0 ) Pub Date : 2020-07-29 , DOI: 10.1002/cplu.202000516
Ramdas Nishanth Rao 1 , Rajeeva Lochana Panchangam 2 , Venkatraman Manickam 2 , Musuvathi Motilal Balamurali 3 , Kaushik Chanda 1
Affiliation  

In this work, a series of novel C−N cyclometalated 2H‐indazole Ru(II) and Ir(III) complexes were synthesized, wherein chelating ligands with substituents like H, and isopropyl group in the R4 position of the phenyl ring of the 2H‐indazole chelating ligand are present. The cytotoxicity of Ru(II) and Ir(III) complexes has been evaluated against different human cancer cell lines (HeLa, MCF‐7, and A549) in a concentration‐dependent manner. The new iridium complex with isopropyl substituent in the phenyl ring of the 2H‐indazole moiety showed good cytotoxic activity against MCF‐7 cells with an IC50 value 3.5 μM. The complex also exhibited cytotoxicity comparable to that of cisplatin. The ability of this compound inducing apoptosis was tested by nuclear condensation, cell membrane blebbing and caspase 3/7 activation. Further, this iridium complex is capable of inhibiting cancer cell migration when tested in MCF‐7 cell line. Subsequently, we have studied the DNA binding and protein binding ability of the newly synthesized iridium complex.

中文翻译:

环金属化2H-吲唑钌(II)和铱(III)配合物的合成及抗肿瘤活性评估。

在这项工作中,合成了一系列新型的CN环金属化的2 H-吲唑Ru(II)和Ir(III)配合物,其中螯合的配位体在H的苯环的R 4位具有H和异丙基等取代基。存在2 H-吲唑螯合配体。已经以浓度依赖的方式评估了Ru(II)和Ir(III)复合物对不同人类癌细胞系(HeLa,MCF-7和A549)的细胞毒性。在2 H-吲唑部分的苯环中具有异丙基取代基的新铱配合物对ICF 50的MCF-7细胞具有良好的细胞毒性值3.5μM。该复合物还显示出与顺铂相当的细胞毒性。通过核浓缩,细胞膜起泡和胱天蛋白酶3/7活化测试了该化合物诱导凋亡的能力。此外,当在MCF-7细胞系中进行测试时,这种铱复合物能够抑制癌细胞迁移。随后,我们研究了新合成的铱配合物的DNA结合和蛋白质结合能力。
更新日期:2020-08-21
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