Kumar, AdarshBhagat, Kuber KumarSingh, Ankit KumarSingh, HarshwardhanAngre, TanujaVerma, AmitaKhalilullah, HabibullahJaremko, MariuszEmwas, Abdul-HamidKumar, Pradeep2024-01-212024-08-132024-01-212024-08-132023-03-032046206910.1039/d3ra00056ghttp://10.2.3.109/handle/32116/3595Cancer is a major cause of deaths across the globe due to chemoresistance and lack of selective chemotherapy. Pyrido[2,3-d]pyrimidine is an emerging scaffold in medicinal chemistry having a broad spectrum of activities, including antitumor, antibacterial, CNS depressive, anticonvulsant, and antipyretic activities. In this study, we have covered different cancer targets, including tyrosine kinase, extracellular regulated protein kinases - ABL kinase, phosphatidylinositol-3 kinase, mammalian target of rapamycin, p38 mitogen-activated protein kinases, BCR-ABL, dihydrofolate reductase, cyclin-dependent kinase, phosphodiesterase, KRAS and fibroblast growth factor receptors, their signaling pathways, mechanism of action and structure-activity relationship of pyrido[2,3-d]pyrimidine derivatives as inhibitors of the above-mentioned targets. This review will represent the complete medicinal and pharmacological profile of pyrido[2,3-d]pyrimidines as anticancer agents, and will help scientists to design new selective, effective and safe anticancer agents. � 2023 The Royal Society of Chemistry.en-USAmino acidsAromatic compoundsCell cultureDiseasesDrug productsMammalsAnti-cancer agentsAnti-tumorsAntibacterialsAnticonvulsant activityAntipyretic activitiesBroad spectrumCauses of deathChemoresistanceMedicinal chemistryTyrosine kinaseChemotherapyReviewhttp://xlink.rsc.org/?DOI=D3RA00056G