title: Design and development of oxazol-5-ones as potential partial PPAR-γ agonist against cancer cell lines.
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.
authors.forename: Tanushree
authors.initials: T
authors.lastname: Pal
authors.forename: Hardik
authors.initials: H
authors.lastname: Joshi
authors.affiliation: Bharati Vidyapeeth's College of Pharmacy, Department of Pharmaceutical Chemistry, Sector-8, C.B.D., Belapur Navi Mumbai-400614, Maharashtra, India. sinharamaa@yahoo.in.
authors.forename: C S
authors.initials: CS
authors.lastname: Ramaa
mesh_terms: D000083:Acetanilides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020014:K562 Cells; D007624:KB Cells; D061986:MCF-7 Cells; D015394:Molecular Structure; D009369:Neoplasms / Q000378:metabolism* / Q000473:pathology*; D023303:Oxazolidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D047495:PPAR gamma / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: C000595963:2-(4-(5-oxo-2-phenyloxazol-4-ylidenemethyl)phenoxy)-N-(3-(trifluoromethyl)phenyl)acetamide; D000083:Acetanilides; D000970:Antineoplastic Agents; D023303:Oxazolidinones; D047495:PPAR gamma