Azolo[1,5-a]pyrimidines as a promising platform for the development of antitumour agents. Structure–activity relationship

Malignant tumours are the second leading cause of death among working-age population; meanwhile, prevention and treatment of these diseases is hampered by the wide diversity of cell types that can become malignant or develop resistance to chemotherapy. Recent years have witnessed a considerable growth of the fascination with azolo[1,5-a]pyrimidines as a promising platform for developing antitumour agents; several drugs based on this platform are already in clinical trials or are used in practice. The present review, devoted to this platform, considers the diversity of oncogenic targets that are affected by azolo[1,5-a]pyrimidines and demonstrates their cytotoxic action against various types of cancer cells. The main focus is on the antitumour potential of azole[1,5-a]pyrimidines. Analysis of modern literature including 132 studies reveals the key structure–activity relationships and provides conclusions about the most promising substitution patterns in the heterocyclic system depending on the macromolecular target. The structures of the lead compounds are presented, and the cell lines most sensitive to azolopyrimidines are listed.

The bibliography includes 196 references.