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Published on: December 7, 2014
Benzimidazole-based protein kinase inhibitors: Current perspectives in targeted cancer therapy
Alaa M Ali1, Samar S Tawfik1, Amany S Mostafa1
1Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt.
Abstract:
Targeted therapy has emerged to be the cornerstone of advanced cancer treatment, allowing for more selectivity and avoiding the common drug toxicity and resistance. Identification of potential targets having vital role in growth and survival of cancer cells got much easier with the aid of the recent advances in high throughput screening approaches. Various protein kinases came into focus as valuable targets in cancer therapy. Meanwhile, benzimidazole-based scaffolds have gained significant attention as promising protein kinase inhibitors with high potency and varied selectivity. Great diversity of these scaffolds has inspired the medicinal chemists to inspect the effect of structural changes upon inhibitory activity on the molecular level through modeling studies. The present review gathers all the considerable attempts to develop benzimidazole-based compounds; designed as protein kinase inhibitors with anticancer activity since 2015; that target aurora kinase, CDK, CK2, EGFR, FGFR, and VEGFR-2; to allow further development and progression regarding benzimidazoles.
Insights
Benzimidazole compounds are promising targeted cancer therapies, acting as potent protein kinase inhibitors. This review highlights recent advancements in developing these anticancer agents since 2015.
Area of Science:
- Medicinal Chemistry
- Oncology
- Drug Discovery
Background:
- Targeted cancer therapy offers improved selectivity and reduced toxicity compared to traditional treatments.
- Protein kinases are crucial targets in cancer, and benzimidazole scaffolds show promise as inhibitors.
- High-throughput screening aids in identifying novel cancer targets and therapeutic agents.
Purpose of the Study:
- To review benzimidazole-based compounds developed as protein kinase inhibitors with anticancer activity since 2015.
- To consolidate research on benzimidazoles targeting specific kinases like aurora kinase, CDK, CK2, EGFR, FGFR, and VEGFR-2.
- To provide insights for future development of benzimidazole-based anticancer drugs.
Main Methods:
- Literature review of scientific publications from 2015 onwards.
- Focus on benzimidazole derivatives designed as protein kinase inhibitors.
- Analysis of targeted kinases including aurora kinase, CDK, CK2, EGFR, FGFR, and VEGFR-2.
Main Results:
- Benzimidazole scaffolds are versatile and have yielded potent inhibitors for various protein kinases.
- Structural modifications of benzimidazoles influence their inhibitory activity and selectivity.
- Significant progress has been made in developing benzimidazole-based anticancer agents.
Conclusions:
- Benzimidazole derivatives represent a valuable class of compounds for targeted cancer therapy.
- Further research into structure-activity relationships can optimize benzimidazole-based kinase inhibitors.
- These compounds hold potential for the development of next-generation anticancer drugs.
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