Synthesis and anticancer activity evaluation of N-[4-(2-methylthiazol-4-yl)phenyl]acetamide derivatives containing (benz)azole moiety

YURTTAŞ L., ÖZKAY Y., AKALIN ÇİFTÇİ G., Ulusoylar-Yildirim S.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol.29, no.2, pp.175-184, 2014 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 29 Issue: 2
  • Publication Date: 2014
  • Doi Number: 10.3109/14756366.2013.763253
  • Journal Name: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.175-184
  • Keywords: A549, anticancer activity, benz(azole), C6, thiazole, BENZIMIDAZOLE DERIVATIVES, ANTIPROLIFERATIVE ACTIVITY, BIOLOGICAL EVALUATION, DNA-BINDING, AGENTS, ANTITUMOR, THIAZOLE, TIAZOFURIN, BENZOXAZOLES, DOXORUBICIN
  • Anadolu University Affiliated: Yes

Abstract

A new class of novel thiazole-(benz) azole derivatives was synthesized to investigate their anticancer activity. The structure of the compounds was confirmed by IR, H-1-NMR, and MS spectral data and elemental analyses. Anticancer effect of the compounds was evaluated against A549 and C6 tumor cell lines. MTT, analysis of DNA synthesis, acridine orange/ethidium bromide staining method and analysis of caspase-3 activation assays were performed for anticancer activity investigations. Compounds 6f and 6g, which carry 5-chloro and 5-methylbenzimidazole groups showed significant anticancer activity. Potential of these compounds to direct tumor cells to apoptotic pathway, which is a precondition of anticancer action, was also observed.