Identification of a New Pentafluorosulfanyl-Substituted Chalcone with Activity Against Hepatoma and Human Parasites
Background/Objectives: New drugs are required for the treatment of liver cancers and protozoal parasite infections. Analogs of the known anticancer active and antileishmanial 2′,4′,6′-trimethoxychalcone SU086 were prepared and investigated. Methods: The chalcones were prepared according to the Clais...
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| Main Authors: | , , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2025-01-01
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| Series: | Pharmaceuticals |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1424-8247/18/1/50 |
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| Summary: | Background/Objectives: New drugs are required for the treatment of liver cancers and protozoal parasite infections. Analogs of the known anticancer active and antileishmanial 2′,4′,6′-trimethoxychalcone SU086 were prepared and investigated. Methods: The chalcones were prepared according to the Claisen–Schmidt condensation protocol and analyzed. They were tested for activity against two liver cancer cell lines (HepG2 and HuH-7) and protozoal parasites (<i>Toxoplasma gondii</i> and <i>Leishmania major</i>). Unspecific toxicity and expression of Hsp90 and Hsp70 upon treatment were analyzed in liver cancer cells. Results: A new chalcone, 2′,4′,6′-trimethoxy-3-pentafluorosulfanylchalcone (246TMP-3SF5), with a pentafluorosulfanyl (SF<sub>5</sub>) substituent showed pronounced activities against liver cancer cells and <i>T. gondii</i> parasites which were superior to the activities of the parent chalcone SU086 in these models. In contrast, SU086 and its anthracene analog 2′,4′,6′-trimethoxy-9-anthracenylchalcone (246TMP-Anth) were most active against <i>L. major</i> promastigotes. The new SF<sub>5</sub>-substituted chalcone behaved like the known Hsp90 inhibitor 17-AAG and upregulated Hsp70 expression in liver cancer cells. Conclusions: The SF<sub>5</sub>-substituted SU086 analog has potential to become a new drug for the therapy of hepatoma and toxoplasmosis. |
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| ISSN: | 1424-8247 |