Evaluation of newly synthesized derivatives of bis(hydrazine‐1‐carbothioamide) and their metal complexes synthesized in bulk and nano size as potent anticancer agents

• Published in: Applied organometallic chemistry Vol. 33; no. 11
• Main Authors: Taha, Rania H., Saleh, Nashwa M., Elhady, Heba A., Khodairy, Manal M.
• Format: Journal Article
• Language: English
• Published: Chichester Wiley Subscription Services, Inc 01.11.2019
• Subjects: Anticancer properties; Biotechnology; bis(hydrazine‐1‐carbothioamide); Cancer; Chemistry; Coordination compounds; Electron microscopy; Electronic spectra; Gallium; Halides; HCT‐116 cell line; HepG2 cell line; Hydrazines; Magnetic moments; Metal halides; Metals; Microscopy; nano complexes; Nitrates; Synthesis; thiosemicarbazide; Zinc chloride
• ISSN: 0268-2605; 1099-0739
• DOI: 10.1002/aoc.5207

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. New metal complexes of bis(hydrazine‐1‐carbothioamide) were synthesized in both bulk and nano‐size and evaluated as anti‐cancer agents against two cell lines human hepatocellular carcinoma (HepG2) and human colorectal carcinoma (HCT‐116). The inhibitory effects showed that most of the tested compounds have higher activity than the standard especially the nano‐size complexes.