About this Research Topic

Background

In the field of medicinal chemistry, heterocyclic compounds play an essential role by displaying different biological activity. Five-membered ring containing heterocycles always attracted researchers due to their versatile diversified biological activities. Heterocyclic scaffolds not only offer opportunities to enhance the drug's permeability through the plasma membrane by increasing its lipophilicity but also have the potential to improve aqueous solubility, leading to its enhanced bioavailability. Five-membered ring heterocycles such as imidazole indole, pyrazole, oxadiazole, thiadiazole, and triazole represent the key heterocyclic structural motifs found in a variety of drugs that are currently in clinical use. The past three years have witnessed several FDA approved heterocyclic drugs for the cancer treatment. Some of the anticancer drugs containing different heterocyclic scaffolds recently approved by FDA. Despite tremendous progress in recent years, more effective and selective targeted small-molecule agents are desperately needed to fight against cancers and combat multidrug resistance (MDR).

Despite the wide range of biological activities and anticancer activity of five-membered ring heterocyclic and related-compounds, there is still a need for the development of novel, practical, and efficient methods for heterocyclic compound synthesis, which nowadays is an important goal in modern organic synthesis. Selective and targeted anticancer drug research are even more important, especially when we consider increasing drug resistance. Therefore, the development of synthetic or natural five-membered ring heterocyclic compounds and the study of their anticancer properties are of key importance for medicinal chemistry. The aim of this Research Topic is to cover promising, recent, and novel research trends in five-membered ring heterocyclic compounds as anticancer drug candidates.

We welcome Original Research, Review, Mini Review and Perspective articles on themes including, but not limited to:
• Synthesis of novel five-membered ring heterocyclic compounds
• Natural compounds containing five-membered ring heterocyclics
• In vitro and in vivo anticancer investigations
• Computer-aided drug design and calculations
• Heterocyclic compound-conjugated macromolecules

Keywords: Five-membered ring heterocycles, Anticancer, CADD, Synthesis, Drug candidates

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