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Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
DOI: 10.2174/15701808113106660080      Price:  $58

Synthesis and Anti-Proliferative Activity of New Biphenyle-Benzylidenethiazolidine- 2,4-dione Bis-Adducts Containing Various Heterocyclic Cores

Author(s): Maxime Meyer, Sandra Kuntz, Isabelle Grillier-Vuissoz, Helene Martin, Lysiane Richert, Stephane Flament, Yves Chapleur and Michel Boisbrun
Pages 256-264 (9)
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.
Cancer, Chromane, Hepatotoxicity, Imidazole, Thiazolidine-2, 4-dione, Triazole, Troglitazone.
SRSMC, UMR 7565, BP 70239, F-54506 Vandoeuvre-les-Nancy, France.