Synthesis of Some 2-Substituted-5-(Benzothiazol-2-yl)-1H-Benzimidazole Derivatives and Investigation of Their Antiproliferative Effects

Polat B. U., Cevik U., DİKMEN M., ÖZKAY Y.

PHARMACEUTICAL CHEMISTRY JOURNAL, vol.56, no.4, pp.451-455, 2022 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 56 Issue: 4
  • Publication Date: 2022
  • Doi Number: 10.1007/s11094-022-02658-3
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, BIOSIS, Biotechnology Research Abstracts, Chemical Abstracts Core, EMBASE
  • Page Numbers: pp.451-455
  • Keywords: cancer, cytotoxicity, benzimidazole, benzothiazole, Cisplatin, synthesis, BIOLOGICAL EVALUATION, ANTITUMOR-ACTIVITY, BENZOTHIAZOLE, INHIBITORS, APOPTOSIS, DESIGN
  • Anadolu University Affiliated: Yes


In addition to methods such as radiotherapy and surgery, another effective way that is preferred for the treatment of cancer is based on the use of chemotherapeutic agents. Although there are more than hundred drugs for cancer treatment, there is still a need to develop new anticancer drugs because of reasons such as drug resistance, side effects, low selectivity and severe toxicity. Benzimidazole and benzothiazole ring systems are the basis of chemical structures of many important drugs because of their different pharmacological properties. In this work, due to potential anticancer effects of benzothiazole and benzimidazole ring systems, eight new compounds that contain both these ring systems in the same chemical structure were synthesized. The structures of obtained compounds were characterized by the IR, NMR, and mass spectroscopy and by elemental analysis data. Cytotoxic effects of the synthesized compounds were tested on Caco-2 (ATCC HTB-37), A549 (ATCC CCL-185) and NIH3T3 (ATCC CRL-1658) cell lines. Two compounds (3c and 3e) were determined as the most effective agents that showed activity comparable with that of the reference drug Cisplatin.