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

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

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 14 , Issue 6 , 2014

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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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Article Details

Year: 2014
Published on: 11 June, 2014
Page: [872 - 883]
Pages: 12
DOI: 10.2174/1871520614666140528155118
Price: $65

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