Synthesis and antiproliferative activity evaluation of new thiazole-benzimidazole derivatives using real-time cell analysis (RTCA DP)

ÖZKAY Y., YURTTAŞ L., DİKMEN M., Engur S.

MEDICINAL CHEMISTRY RESEARCH, vol.25, no.3, pp.482-493, 2016 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 25 Issue: 3
  • Publication Date: 2016
  • Doi Number: 10.1007/s00044-016-1507-0
  • Journal Name: MEDICINAL CHEMISTRY RESEARCH
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.482-493
  • Keywords: Thiazole, Benzimidazole, Cytotoxic activity, Anticancer activity, Antiproliferative activity, Real-time cell analysis (RTCA), xCELLigence, ANTITUMOR-ACTIVITY, DNA-BINDING, POTENTIAL ANTITUMOR, CANCER, AGENTS, INHIBITORS, BLEOMYCIN, CLEAVAGE, ENHANCEMENT, THERAPY
  • Anadolu University Affiliated: Yes

Abstract

A series of new 2-[(5-substituted-1H-benzimidazol-2-yl)thio]-N-[4-[2-phenylthiazol-4-yl]phenyl]acetamide derivatives (4a-p) were synthesized according to the reported literature, and anticancer activity of the compounds was evaluated. Cytotoxic activity was confirmed by real-time cytotoxicity analysis system determining half maximal inhibitory concentrations (IC50) of the title compounds based on the dose-response curves derived by xCELLigence measurements against NIH/3T3, A549 and Caco2 cell lines for 24, 48 and 72 h exposure. Compound 4c was found to be as the most efficient molecule that exhibited selective antiproliferative activity against both of the cancer cells.