Anticancer benzimidazole derivatives as inhibitors of epigenetic targets: a review article

Area of Science:

• Oncology
• Epigenetics
• Medicinal Chemistry

Background:

• Cancer remains a major global health challenge, with epigenetic dysregulation significantly contributing to its development and progression.
• Epigenetic modifications, which alter gene expression without changing DNA sequence, are increasingly recognized as critical therapeutic targets.
• Targeting epigenetic mechanisms offers a promising avenue for developing novel, less toxic cancer treatments.

Purpose of the Study:

• To provide a comprehensive review of benzimidazole derivatives as epigenetic modulators in cancer therapy.
• To highlight the therapeutic potential of benzimidazole derivatives targeting DNA methyltransferases, histone deacetylases, and histone methyltransferases.
• To emphasize recent advancements and future directions for benzimidazole-based epigenetic drugs in oncology.

Main Methods:

• Literature review focusing on benzimidazole derivatives and their interaction with epigenetic targets (readers, writers, erasers).
• Analysis of studies investigating the efficacy of benzimidazole derivatives in preclinical and clinical cancer models.
• Synthesis of information on the mechanisms of action and therapeutic potential of these compounds.

Main Results:

• Benzimidazole derivatives exhibit potent inhibition of key epigenetic targets involved in cancer.
• Several promising benzimidazole derivatives are advancing through clinical trials for hematological and solid malignancies.
• These compounds demonstrate potential for developing targeted, less toxic cancer therapies.

Conclusions:

• Benzimidazole derivatives represent a valuable class of epigenetic agents for cancer treatment.
• Further research into benzimidazole derivatives could lead to the design of multi-target drugs to overcome resistance and improve clinical outcomes.
• This review serves as a resource for researchers developing novel anticancer benzimidazole derivatives with enhanced properties.