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Description:

Hepatocellular carcinoma (HCC) is one of the leading causes of cancer-related morbidity
worldwide. Sorafenib is a first-line drug for the treatment of HCC, however, it is reported to
cause serious adverse effects and may lead to resistance in many patients. In this study, 20
hydrazone derivatives incorporating triazoles, pyrazolone, pyrrole, pyrrolidine, imidazoline,
quinazoline, and oxadiazine moieties were designed, synthesized, and characterized. In
addition to molecular docking and in silico ADME study, the cytotoxic activity of the
synthesized compounds was evaluated against the human hepatocellular cancer cell line
(HepG2) and liver mesenchymal stem cells as a normal cell line. The antitumor activities of
the derivatives against sorafenib were compared. Of the 20 synthesized compounds,
compound 16 demonstrated potential as a potent anti-HCC drug candidate through
downregulation of interleukin 6 which reduces inflammation and tumorigenesis with a strong
binding interaction and bioavailability.

Rights:

• https://creativecommons.org/licenses/by/3.0/legalcode
  

Keyword: HCC, IL-6, hydrazone derivatives, antitumor, cytochrome c, molecular docking simulation, Sorafenib, 5-fluoruracil, hepatocellular carcinoma.

Date published: 2024-11-28

Publisher: Royal Society of Chemistry (RSC)

Journal:

• RSC Advances (ISSN: 20462069) vol. 14 issue. 51 p. 37960-37974

Funding:

• American University in Cairo

Manuscript type: Publisher's version (Version of record)

MDR DOI:

First published URL: https://doi.org/10.1039/d4ra05854b

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Updated at: 2024-12-04 14:53:06 +0900

Published on MDR: 2024-12-04 14:53:06 +0900