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Evaluation of newly synthesized derivatives of bis(hydrazine‐1‐carbothioamide) and their metal complexes synthesized in bulk and nano size as potent anticancer agents
Authors:Rania H Taha  Nashwa M Saleh  Heba A Elhady  Manal M Khodairy
Abstract:A series of new metal complexes were synthesized in both bulk and nano size using green methods, starting with the reaction of (E)‐N′‐(E)‐2‐bromobenzylidene]‐4‐oxo‐4‐(piperidin‐1‐yl)but‐2‐enehydrazide with thiosemicarbazide and different metal halides such as CuI·2H2O, CuCl2·2H2O, CoCl2·2H2O, and ZnCl2·2H2O, and metal nitrate such as Ga(NO3)3·2H2O. Structures of these metal complexes were confirmed using different spectroscopic methods, elemental analysis, electronic spectra, and microanalytical methods (scanning electron microscopy and transmission electron microscopy) for nano complexes. The distorted octahedral geometry for all complexes was suggested based on magnetic moments and electronic spectral studies. The cytotoxic activity of the compounds was investigated against human hepatocellular carcinoma (HepG2) and human colorectal carcinoma (HCT‐116) cell lines. Most tested compounds had higher inhibitory activity than the standard vinblastine drug. Interestingly, the nano‐sized Ga(III) complex 11 was the most potent compound against the two tested cell lines, with 50% inhibitory concentration (IC50) of 2.56 μg/mL for HepG2, compared with the reference drug vinblastine (IC50 15.6 μg/mL), and IC50 4.64 μg/mL for HCT‐116, compared with the standard (IC50 13.9 μg/mL). The bioassay results helped us identify new potent and selective anticancer agents.
Keywords:bis(hydrazine‐1‐carbothioamide)  HCT‐116 cell line  HepG2 cell line  nano complexes  thiosemicarbazide
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