Design and Development of Oxazol-5-Ones as Potential Partial PPAR-gamma Agonist Against Cancer Cell Lines

作者：Pal Tanushree; Joshi Hardik; Ramaa C S^*

来源：Anti-Cancer Agents in Medicinal Chemistry, 2014, 14(6): 872-883.

DOI：10.2174/1871520614666140528155118

• Akt/mTOR/p70S6 signalling
• Cancer
• Sulforhodamine B

Recent era aims at developing safer partial Peroxisome proliferator-activated receptor-gamma (PPAR- gamma) agonists in order to dodge the toxicity issues related to full agonists. With a view to develop non-thiazolidinediones as partial PPAR-gamma agonists, novel analogues of oxazol-5-ones (3a-3q) were designed and virtually analyzed for their molecular and drug like properties. The newly synthesized compounds were further evaluated for their preliminary cytotoxicity in a panel of eight cancer cell lines using four concentrations at 10-fold dilutions. Sulforhodamine B (SRB) protein assay was used to estimate cell stability or growth. All the compounds demonstrated distinct effect in the extent of cytotoxicity in the breast cancer cell line MCF-7 with 3g specifically exhibiting partial PPAR-gamma agonist activity and adipogenesis stimulating ability.

• 出版日期2014