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Journal of Personalized Medicine

Journal of Personalized Medicine

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Novel Thienyl-Based Tyrosine Kinase Inhibitors for the Treatment of Hepatocellular Carcinoma

Published:1 May 2022 DOI: 10.3390/jpm12050738
Andi Ma,?B. Biersack,?Nils Goehringer,?B. Nitzsche,?M. H?pfner

Abstract

New medical treatments are urgently needed for advanced hepatocellular carcinoma (HCC). Recently, we showed the anticancer effects of novel thiophene-based kinase inhibitors. In this study, we further characterized the antineoplastic effects and modes of action of the two most promising inhibitors, Thio-Iva and Thio-Dam, and compared their effects with the clinically relevant multi-kinase inhibitor, sorafenib, in HCC cells. Crystal violet staining and real-time cell growth monitoring showed pronounced antiproliferative effects in Huh-7 and SNU-449 cells with IC50 values in the (sub-)micromolar range. Long-term incubation experiments revealed the reduced clonogenicity of Thio-Iva and Thio-Dam-treated HCC cells. LDH-release tests excluded cytotoxicity as an unspecific mode of action of the inhibitors, while flow cytometry analysis revealed a dose-dependent and pronounced G2/M phase cell cycle arrest and cyclin B1 suppression. Additionally, mitochondria-driven apoptosis was observed through the cytosolic increase of reactive oxygen species, a concomitant PARP cleavage, and caspase-3 induction. Both compounds were found to effectively inhibit the capillary tube formation of endothelial EA.hy926 cells in vitro, pointing towards additional antiangiogenic effects. Antiangiogenic and antineoplastic effects were confirmed in vivo by CAM assays. In summary, the thienyl-acrylonitrile derivatives, Thio-Iva and Thio-Dam, exert significant antineoplastic and antiangiogenic effects in HCC cells.

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Materials Related products
Procduct Name CAS Molecular Formula Supplier Price
Sorafenib 284461-73-0 C21H16ClF3N4O3 658 suppliers $8.00-$1529.00
Sorafenib 284461-73-0 C21H16ClF3N4O3 658 suppliers $8.00-$1529.00
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Sorafenib 284461-73-0 - Inquiry
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2-?Pyridinecarboxamide, 4-?[4-?[[[[4-?chloro-?3-?(trifluoromethyl)?phenyl]?amino]?carbonyl]?amino]?phenoxy]?-?N-?methyl- 284461-73-0 - Inquiry
2-?Pyridinecarboxamide, 4-?[4-?[[[[4-?chloro-?3-?(trifluoromethyl)?phenyl]?amino]?carbonyl]?amino]?phenoxy]?-?N-?methyl- 284461-73-0 - Inquiry

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