title: Synthesis of Diflunisal Thiazolidinones as Anticancer Agents.
abstract: A series of diflunisal 4-thiazolidinones were synthesized. Some selected compounds were determined at one dose towards the full panel of 60 human cancer cell lines by National Cancer Institute. 2',4'-Difluoro-4-hydroxy-N-[4-oxo-2-(thiophen-2-yl)-1,3-thiazolidin-3-yl]biphenyl- 3-carboxamide (4a) demonstrated the most marked effect on K-562 cancer cell line with 58.59 % growth inhibition at 10 μM. Compound 4a was evaluated in vitro using the MTT colorimetric method against human leukemia cell line K-562 and mouse embryonic fibroblasts cell line NIH- 3T3 at different doses for cell viability and growth inhibition. Compound 4a exhibited anticancer activity with IC50 value of 5.2 μM against K-562 cells and did not display cytotoxicity towards NIH-3T3 cells compared with diflunisal. In addition, this compound could be an interesting prototype as an antiproliferative agent.
authors: Sevil
authors: S
authors: Şenkardeş
authors: Özlem B
authors: ÖB
authors: Özakpınar
authors: Derya
authors: D
authors: Özsavcı
authors: Azize
authors: A
authors: Şener
authors: Özge
authors: Ö
authors: Çevik
authors: Marmara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Haydarpaşa 34668 İstanbul, Turkey. gkucukguzel@marmara.edu.tr.
authors: Ş Güniz
authors: ŞG
authors: Küçükgüzel
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D060326:Chemistry Techniques, Synthetic; D004061:Diflunisal / Q000737:chemistry* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020014:K562 Cells / Q000187:drug effects; D051379:Mice; D041681:NIH 3T3 Cells
chemical_list: D000970:Antineoplastic Agents; D004061:Diflunisal