Dual‐Targeting Strategy in Cancer Therapy: The Emerging Role of Pyrrolopyrimidine Scaffolds

Abstract

Pyrrolopyrimidine has emerged as a privileged scaffold in medicinal chemistry, owing to its synthesis with variable substitutions and the capacity to exhibit potent, diverse pharmacological profiles. In recent years, the development of dual-target agents has emerged as a research hotspot in cancer therapy, driven by their ability to overcome drug resistance, enhance pharmacokinetic and safety profiles, and improve patient compliance. The current review focuses on the concept of dual-targeted anticancer agents, with particular emphasis on pyrrolopyrimidine-based compounds capable of simultaneously modulating two distinct targets within cancer cells. Furthermore, it highlights resistance mechanisms, development strategies, target mechanisms, in vitro activity profiles, in vivo efficacy data, and available clinical findings, providing a comprehensive overview of their therapeutic potential and future prospects in oncology.