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.
Anti-Cancer Agents in Medicinal Chemistry
Title:Design and Development of Oxazol-5-Ones as Potential Partial PPAR-γ Agonist Against Cancer Cell Lines
Volume: 14 Issue: 6
Author(s): Tanushree Pal, Hardik Joshi and C.S. Ramaa
Affiliation:
Keywords: Akt/mTOR/p70S6 signalling, Cancer, Sulforhodamine B.
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.
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Pal Tanushree, Joshi Hardik and Ramaa C.S., Design and Development of Oxazol-5-Ones as Potential Partial PPAR-γ Agonist Against Cancer Cell Lines, Anti-Cancer Agents in Medicinal Chemistry 2014; 14 (6) . https://dx.doi.org/10.2174/1871520614666140528155118
DOI https://dx.doi.org/10.2174/1871520614666140528155118 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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