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Pyrido[2,3-<i>d</i>]pyrimidines (<b>1</b>) are a type of privileged heterocyclic scaffolds capable of providing ligands for several receptors in the body. Among such structures, our group and others have been particularly interested in pyrido[2,3-<i>d</i>]pyrimidine-7(8<i>H</i>)-ones (<b>2</b>) due to the similitude with nitrogen bases present in DNA and RNA. Currently there are more than 20,000 structures <b>2</b> described which correspond to around 2900 references (half of them being patents). Furthermore, the number of references containing compounds of general structure <b>2</b> have increased almost exponentially in the last 10 years. The present review covers the synthetic methods used for the synthesis of pyrido[2,3-<i>d</i>]pyrimidine-7(8<i>H</i>)-ones (<b>2</b>), both starting from a preformed pyrimidine ring or a pyridine ring, and the biomedical applications of such compounds.