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Anti-Cancer Agents in Medicinal Chemistry


ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Research Article

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

Author(s): Tanushree Pal, Hardik Joshi and C.S. Ramaa

Volume 14, Issue 6, 2014

Page: [872 - 883] Pages: 12

DOI: 10.2174/1871520614666140528155118

Price: $65


Recent era aims at developing safer partial Peroxisome proliferator-activated receptor-γ (PPAR- γ) agonists in order to dodge the toxicity issues related to full agonists. With a view to develop non-thiazolidinediones as partial PPAR-γ 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-γ agonist activity and adipogenesis stimulating ability.

Keywords: Akt/mTOR/p70S6 signalling, Cancer, Sulforhodamine B.

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