Facile synthesis of C6-substituted benz[4,5]imidazo[1,2-a]quinoxaline derivatives and their anticancer evaluation

Rahul Singh, Ravinder Kumar, Mallesh Pandrala, Parleen Kaur, Saloni Gupta, Dhanir Tailor, Sanjay V. Malhotra, Deepak B. Salunke

Research output: Contribution to journalArticlepeer-review

4 Scopus citations


Cancer remains a leading cause of death worldwide, resulting in continuous efforts to discover and develop highly efficacious anticancer drugs. High-throughput screening of heterocyclic compound libraries is one of the promising approaches that provided several new lead molecules with a novel mechanism of action. On the basis of the promising anticancer potential of imidazoquinoxaline as well as the structurally similar imidazoquinoline-derived scaffold, we prepared a set of C6-substituted benzimidazo[1,2-a]quinoxaline derivatives via two novel synthetic routes using commercially available starting materials, with good to excellent yields and evaluated their anticancer activity against the NCI-60 cancer cell lines. The one-dose (10 µM) anticancer screening of the synthesized compounds in the NCI-60 cell line panel revealed that the substituents have a significant role in the activity. In particular, the indole (7f), imidazole (7g), and benzimidazole (7h) derivatives showed significant activity against the triple-negative breast cancer cell line, MDA-MB-468. The lead compounds also exhibited notable IC50 values against another breast cancer cell line, MCF-7. Furthermore, it was observed that these compounds were relatively nontoxic to normal cell lines: HEK293 (human embryonic kidney cell line) and MCF12A (nontumorigenic human breast epithelial cell line). The IC50 values against healthy cells were at least 5- to 11-fold higher, offering a new class of heterocycles that can be further developed as promising therapeutics for cancer treatment.

Original languageEnglish (US)
Article number2000393
JournalArchiv der Pharmazie
Issue number7
StatePublished - Jul 2021


  • MDA-MB-468
  • NCI-60
  • anticancer agents
  • benzimidazole
  • breast cancer cell line
  • heterocycles
  • quinoxaline

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery


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