Synthesis of Diflunisal Thiazolidinones as Anticancer Agents

ŞENKARDEŞ S., BİNGÖL ÖZAKPINAR Ö., ÖZSAVCI D., ŞENER A., Cevik O., KÜÇÜKGÜZEL Ş. G.

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY, cilt.16, sa.10, ss.1266-1274, 2016 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 16 Sayı: 10
  • Basım Tarihi: 2016
  • Doi Numarası: 10.2174/1871520615666150831125337
  • Dergi Adı: ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.1266-1274
  • Anahtar Kelimeler: Annexin-V, apoptosis, diflunisal, K-562 cancer cell line, 4-Thiazolidinone, NATIONAL-CANCER-INSTITUTE, HYDRAZIDE-HYDRAZONES, CASPASE ACTIVATION, DRUG DISCOVERY, APOPTOSIS, CYTOTOXICITY, DERIVATIVES, MECHANISMS, SCREEN, CELLS
  • Marmara Üniversitesi Adresli: Evet

Özet

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 mu M. 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 mu M 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.