کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1392420 | 1501133 | 2014 | 12 صفحه PDF | دانلود رایگان |
• Synthesis of new troglitazone derivatives is reported.
• Anti-proliferative activity against breast cancer cell lines showed low micromolar potency.
• Low cytotoxicity towards primary cultured non-malignant human hepatocytes was observed.
Δ2-Troglitazone derivatives were shown to exhibit anti-proliferative activity in a PPARγ-independent manner. We prepared various compounds in order to increase their potency and decrease their toxicity towards non-malignant primary cultured hepatocytes. Many compounds induced viabilities less than 20% at 10 μM on various cancer cell lines. Furthermore, five of them showed hepatocyte viability of 80% or more at 200 μM. In addition, compounds 17 and 18 exhibited promising maximum tolerated doses on a murine model, enabling future investigations.
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Journal: European Journal of Medicinal Chemistry - Volume 83, 18 August 2014, Pages 129–140