Hybrid and Chimieric Heterocyclic Compounds as Anticancer and Antimicrobial Agents

Dear Colleagues,

Cancer is among the most merciless, serious and life-threatening diseases worldwide, and is characterized by the uncontrolled and rapid pathological growth of abnormal cells in the body and their spread to different organs (metastasis). According to the World Health Organization (WHO), cancer continues to proliferate around the world, becoming the second leading cause of death worldwide (with over 10 million deaths in 2020) and exerting a great pressure on health systems, individuals and communities. The prevalence of infectious diseases caused by microorganisms (bacteria, fungi, bacillus, etc.) has increased dramatically in recent years and represents a serious threat to public health, killing thousands of people worldwide annually. In particular, the overconsumption, widespread use and misuse of antimicrobial agents have resulted in the emergence of drug resistance, multi-drug resistance and extensive drug resistance to microbial pathogens. Despite the significant advances achieved in both cancer and microbial therapy, the existing treatment options suffer from some major limitations, including drug resistance, multi-drug resistance, extensive drug resistance, the often high toxicity levels and non-specificity of drugs, and their high price, among others. On the other hand, cancer and microbial illnesses are multifactorial diseases that are difficult to treat with drugs that act on a single target. A strategy employed in cancer and microbial therapy is to design Multiple Targeting Drugs, in which a single chemical entity interacts with two or more distinct biological targets related to a disease. These types of drugs are usually classified as either Hybrid Drugs (HD) or Chimeric Drugs (CD). Thus, the continued search for innovative and enhanced anticancer and antimicrobial drugs remains crucial in medicinal chemistry.

A literature survey revealed that among heterocycles are privileged scaffolds applicable to the development of new drug entities, exerting a large variety of biological activities, such as anticancer, antiplasmodial and antimalarial, antitubercular, antibacterial, antifungal, antiviral, anthelmintic, anti-HIV, analgesic, anticonvulsant, anti-inflammatory, antihistaminic, antipsychotic, anti-Alzheimer’s and antihypertensive actions, among others.

The aim of this Special Issue is to provide a platform for researchers to present the latest developments in anticancer and antimicrobial medicinal chemistry research, focused on biological active hybrid and chimieric heterocycles derivatives. 

Prof. Dr. Ionel Mangalagiu
Guest Editor

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• hybrid heterocyclic compounds
• chimieric heterocyclic compounds
• anticancer agents
• antimicrobial agents
• multifactorial diseases
• multiple targeting drugs