Synthesis and Antitumor Activity Evaluation of Cyclometalated 2H‐Indazole Ruthenium(II) and Iridium(III) Complexes

Abstract

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.

Chemical Characterization and Biological Evaluation of New Cobalt(II) Complexes with Bioactive Ligands, 2-Picolinehydroxamic Acid and Reduced Schiff Base N-(2-Hydroxybenzyl)alanine, in Terms of DNA Binding and Antimicrobial Activity

“…The binary Co(II)-AlaSal complexes were equally active against both strains, while AlaSal alone showed lower activity [26]. This is most likely due to the formation of chelates with greater lipophilicity and permeability through the bacterial cell membrane [55]. In turn, PicHA alone, as an inhibitor of bacterial urease [56], exhibits similar MIC values against H. pylori as the heteroligand complexes, and has higher activity against these strains than the binary Co(II)-PicHA complexes [25].…”

The Role of Nanocrystal Facets in Sustainable Organic Synthesis

“…Our research group has also contributed by synthesizing 1 H ‐tetrazole using CuO nanoparticles [43] . Later, we demonstrated the use of Cu 2 O rhombic dodecahedra nanocrystals in 2 H ‐Indazole synthesis [44] which were further utilized for the synthesis of Ruthenium(II) and Iridium(II) metal complexes with potent antitumor activity [45] . The utilisation of polyhedral metal nanocrystals in organic synthesis is gradually increasing due to their environmental sustainability [46] …”

Therapeutic Inhibitory Activities of N‐Hydroxy Derived Cytidines: A Patent Overview

“…[21][22][23][24][25] Recently, we have reviewed on the synthesis of rufinamide, an antiepileptic drug. [26] In continuation of our interest on the synthesis and biological activity of organic compounds, [27][28][29] this review covers the therapeutic patents in the last decade period from 2010-2020.…”