eng Oriental Scientific Publishing Company Biosciences Biotechnology Research Asia 0973-1245 2025-09-30 22 3 849 863 10.13005/bbra/3409 55763 article Deepali Dattatraya Wagh 1 Rani Shantaram Kankate 1 Department of Pharmaceutical Chemistry, MET’s Institute of Pharmacy, Nashik. Savitribai Phule Pune University, Maharashtra, India. Benzimidazole is a compound with significant therapeutic promise, as numerous biochemical and pharmacological studies have highlighted its potent anticancer activity and its potential as a lead scaffold in cancer drug development.  From academic articles to patents, this review covers it everything when it comes to synthetic pathways towards anticancer drugs including benzimidazole.  We have mainly concentrated on the construction of the heterocyclic core and  incorporating benzimidazole due to the large number of possible configurations.  Targeting benzimidazole, one of the most representative chemical entities, is essential.  There has been a recent uptick in interest and focus from academics all over the globe in this area.  Nevertheless, obstacles such as resistance to drugs, a lack of understanding of receptor structures, and difficulties in finding practical ways to synthesize benzimidazoles persist.  As such, we are writing this review in the hopes that it will serve as a thorough resource for future scholars interested in benzimidazole-containing anticancer drugs and drug design. https://www.biotech-asia.org/vol22no3/benzimidazole-derivatives-in-anticancer-therapy-a-comprehensive-review/ Anticancer agents; Benzimidazoles; Drug design; Molecular targets; and Structure-activity relationship