Design and synthesis of indole-benzimidazole hybrid molecules and evaluation of their in-vitro cytotoxic activities

Abstract

ABSTRACT. Cancer is one of the most deadly diseases worldwide, challenging the world for effective treatment of the diseases, to tackle this problem a vast amount of therapeutic candidates are being investigated. Indole-benzimidazole structures have recently gained considerable attention, because compounds containing these structure exhibit a very good anticancer property. Two series of novel indole-benzimidazole hybrids molecules viz., 2-(5-substituted-1H-indol-3-yl)-5-substituted-1H-benzo[d]imidazole 5(a-f) and 2-(5-substituted-1-(3-methylbut-2-enyl)-1H-indol-3-yl)-5-substituted-1H-benzo[d]imidazole 6(a-f) were synthesized and characterized by spectroscopic techniques. The twelve target molecules have been investigated for their in-vitro cytotoxic activity against human ovarian carcinoma cells (SKOV-3), human prostate cancer cells (PC-3), human cervical cancer cells (HeLa) and human acute monocytic leukemia cells (THP-1) using MTT assay. Compound; 2-(5-bromo-1H-indol-3-yl)-5-methyl-1H-benzo[d]imidazole (5e) was interesting with IC₅₀ (μM) values of 23.69 (SKOV-3), 73.05 (PC-3), 64.66 (HeLa) and 39.08 (THP-1), respectively.

KEY WORDS: Indole, Benzimidazole, Hybrid molecules, Anticancer activity

Bull. Chem. Soc. Ethiop. 2023, 37(5), 1209-1220.                                                       

DOI: https://dx.doi.org/10.4314/bcse.v37i5.13