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Benzimidazole hybrids as anticancer drugs: An updated review on anticancer properties, structure-activity
Lian-Shun Feng1, Wen-Qi Su1, Jin-Bo Cheng1
1WuXi AppTec Co., Ltd., Wuhan, People's Republic of China.
Abstract:
Cancer, characterized by a deregulation of the cell cycle which mainly results in a progressive loss of cellular differentiation and uncontrolled cellular growth, remains a prominent cause of death across the world. Almost all currently available anticancer agents used in clinical practice have developed multidrug resistance, creating an urgent need to develop novel chemotherapeutics. Benzimidazole derivatives could exert anticancer properties through diverse mechanisms, inclusive of the disruption of microtubule polymerization, the induction of apoptosis, cell cycle (G2/M) arrest, antiangiogenesis, and blockage of glucose transport. Moreover, several benzimidazole-based agents have already been approved for the treatment of cancers. Hence, benzimidazole derivatives are useful scaffolds for the development of novel anticancer agents. In particular, benzimidazole hybrids could exert dual or multiple antiproliferative activities and had the potential to overcome drug resistance, demonstrating the potential of benzimidazole hybrids as potential prototypes for clinical deployment in the control and eradication of cancers. The purpose of the present review article is to provide a comprehensive landscape of benzimidazole hybrids as potential anticancer agents, and the structure-activity relationship as well as mechanisms of action are also discussed to facilitate the further rational design of more effective candidates, covering articles published from 2019 to 2021.
Insights
Benzimidazole hybrids show promise as novel anticancer agents, offering diverse mechanisms to combat drug resistance and cancer growth. This review highlights their potential for developing new cancer therapies.
Area of Science:
- Medicinal Chemistry
- Oncology
- Drug Discovery
Background:
- Cancer is a leading global cause of death, driven by cell cycle deregulation and uncontrolled growth.
- Existing anticancer drugs often face multidrug resistance, necessitating novel therapeutic strategies.
- Benzimidazole derivatives exhibit anticancer properties via multiple mechanisms, including apoptosis induction and cell cycle arrest.
Purpose of the Study:
- To provide a comprehensive overview of benzimidazole hybrids as potential anticancer agents.
- To discuss structure-activity relationships and mechanisms of action for rational drug design.
- To cover relevant research published between 2019 and 2021.
Main Methods:
- Literature review of scientific articles.
- Analysis of structure-activity relationships (SAR) of benzimidazole hybrids.
- Examination of proposed mechanisms of action against cancer cells.
Main Results:
- Benzimidazole derivatives demonstrate significant anticancer potential through various pathways.
- Benzimidazole hybrids can exhibit dual or multiple antiproliferative activities.
- These hybrids show promise in overcoming multidrug resistance in cancer treatment.
Conclusions:
- Benzimidazole hybrids represent a valuable scaffold for developing next-generation anticancer drugs.
- Understanding SAR and mechanisms is crucial for designing more effective benzimidazole-based cancer therapeutics.
- Benzimidazole hybrids hold potential for clinical application in cancer control and eradication.
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