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

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


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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



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

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

Affiliation: Bharati Vidyapeeth’s College of Pharmacy, Department of Pharmaceutical Chemistry, Sector-8, C.B.D., Belapur Navi Mumbai-400614, Maharashtra, India.

Abstract

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

Volume: 14
Issue Number: 6
First Page: 872
Last Page: 883
Page Count: 12
DOI: 10.2174/1871520614666140528155118
Price: $58
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