Nitrogen-containing heterocycles as topoisomerase II inhibitors for targeting cancer: Recent updates

Cancer is a broad word for a set of diseases that can begin in virtually any organ or tissue of the body and spread to other organs. In 2020, cancer was the largest cause of death worldwide, accounting for 10 million fatalities, or one in every six deaths. Nitrogen containing heterocyclic compounds are a massive research focus because it has a unique position and is a cherished source of a wide range of bioactive molecules in medicinal chemistry. Over 75% of the currently accessible market is covered by FDA-approved drugs containing nitrogen moieties. DNA topoisomerase II is a reassuring approach for novel anticancer heterocyclic medicines because it plays a crucial role in DNA metabolism, replication, recombination, and repair. Given the importance of topo II in chemotherapy, there is a pressing necessity to boost topo II or multi-target topo II inhibitors in order to combat drug resistance and minimize toxicity. Following the trend of researching the advancement of effective topo II inhibitors with minimal toxicity, the current review article consolidates a detailed account of nitrogen-containing heterocyclic compounds and categorizes them into different classes based on structural characterization, such pyrimidine, triazine, pyridine, quinazoline, fluoroquinolones, quinones, pyrazoles, quinoline, carbazoles, beta-carboline, quinolone, naphthalimide, acridone, benzoxazole, pyridophenoxazine, pyrrole, piperazine and imidazole, along with their structure activity relationship, mechanistic aspects, and docking studies (wherever appropriate) were explored. We are certain that the current review paper will help future medical researchers investigate prospective topoisomerase inhibitors as anticancer medicines in a variety of clinical settings.

Automated summary

This article summarizes the significance of nitrogen-containing heterocyclic compounds in medicinal chemistry and their structure-activity relationship, mechanism and docking studies. The importance of DNA topoisomerase II in anticancer drugs is emphasized, calling for further research on topo II or multi-target topo II inhibitors to overcome drug resistance and reduce toxicity.