Synthesis and Anti-Proliferative Activity of New Biphenyle-Benzylidenethiazolidine- 2,4-dione Bis-Adducts Containing Various Heterocyclic Cores
In the course of our ongoing program dedicated to the synthesis of anti-proliferative compounds, we prepared
new troglitazone derivatives bearing a biphenyle moiety. The chromane heterocycle was further replaced by imidazole
and triazole derivatives. Many compounds exhibited fair to high activity towards various cancer cell lines. Among them,
compound 17b reduced cell viability leading to only 22-34% viable cells in four cancer cell lines at 10 µM, but unfortunately
also led to a low (13%) cell viability of non-malignant primary cultured human hepatocytes at 200 µM. Interestingly,
compound 11b also reduced cell viability in colon and liver cancer cell lines (29% and 24% cell viability respectively
at 10 µM), but maintained a high cell viability of non-malignant hepatocytes (reaching 71% cell viability at 200
µM), thus exhibiting a huge selectivity.
Keywords: Cancer, Chromane, Hepatotoxicity, Imidazole, Thiazolidine-2, 4-dione, Triazole, Troglitazone.
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