Biological evaluation of imidazopyridine derivatives as potential anticancer agents against breast cancer cells


Medicinal Chemistry Research, vol.31, no.12, pp.2231-2242, 2022 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 31 Issue: 12
  • Publication Date: 2022
  • Doi Number: 10.1007/s00044-022-02984-x
  • Journal Name: Medicinal Chemistry Research
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, BIOSIS, CAB Abstracts, Chemical Abstracts Core, Chimica, EMBASE, Veterinary Science Database
  • Page Numbers: pp.2231-2242
  • Keywords: Imidazo[1, 2-a]pyridine, Anticancer agent, Breast cancer, Suzuki, Acylhydrazone
  • Istanbul Medipol University Affiliated: Yes


Imidazo[1,2-a]pyridine cores have increasing importance in the pharmaceutical industry with their wide range pharmacological activities. In this study, two series of imidazopyridine derivatives were synthesized. It was planned to integrate the pyrimidine ring or N-acylhydrazone (NAH) to the carbon atom at the 3 position of the imidazo[1,2-a]pyridine scaffold. Pyrimidine-containing compounds (9–12) were obtained by palladium-catalyzed coupling reaction (Suzuki reaction), and NAH compounds (13–19) were obtained from the aldehyde intermediate synthesized as a result of the Vilsmeier-Haack reaction. All of the derivatives were evaluated in breast cancer cells for their antiproliferative potential. The pyrimidine-containing compounds did not show active results in both breast cancer cell lines, while the NAH derivatives showed significant results. Among the novel derivatives, compound 15 exhibited the most potent activity against the MCF7 and MDA-MB-231 cell lines with IC50 values of 1.6 and 22.4 μM, respectively. The current study demonstrated that these compounds have anticancer activity and would be useful in developing more effective compounds for treating breast cancer.