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Issue 1, 2017
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Quinoides and VEGFR2 TKIs influence the fate of hepatocellular carcinoma and its cancer stem cells

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Abstract

Bioactivities of quinoides 1–5 and VEGFR2 TKIs 6–10 in hepatocellular cancer (HCC) and cancer stem cells (HCSCs) were studied. The compounds exhibited IC50 values in μM concentrations in HCC cells. Quinoide 3 was able to eradicate cancer stem cells, similar to the action of the stem cell inhibitor DAPT. However, the more cytotoxic VEFGR TKIs (IC50: 0.4–3.0 μM) including sorafenib, which is the only FDA approved drug for the treatment of HCC, enriched the hepatocellular cancer stem cell population by 2–3 fold after treatment. An aggressiveness factor (AF) was proposed to quantify the characteristics of drug candidates for their ability to eradicate the CSC subpopulation. Considering the tumour heterogeneity and marker positive cancer stem cell like subpopulation enrichment upon treatments in patients, this study emphasises the importance of the chemotherapeutic agent choice acting differentially on all the subpopulations including marker-positive CSCs.

Graphical abstract: Quinoides and VEGFR2 TKIs influence the fate of hepatocellular carcinoma and its cancer stem cells

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Publication details

The article was received on 15 Jul 2016, accepted on 27 Sep 2016 and first published on 07 Oct 2016


Article type: Research Article
DOI: 10.1039/C6MD00392C
Citation: Med. Chem. Commun., 2017,8, 81-87
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    Quinoides and VEGFR2 TKIs influence the fate of hepatocellular carcinoma and its cancer stem cells

    D. C. Kahraman, G. Hanquet, L. Jeanmart, S. Lanners, P. Šramel, A. Boháč and R. Cetin-Atalay, Med. Chem. Commun., 2017, 8, 81
    DOI: 10.1039/C6MD00392C

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