Pyrimidine, also known as 1,3-diazobenzene, is a heterocyclic compound with the chemical formula C4H4N2. Pyrimidine is formed by substituting 2 nitrogen atoms for 2 carbons in the meta-position of benzene. It is a diazine and retains its aromaticity. Derivatives of pyrimidine widely exist in organic macromolecular nucleic acids, and many drugs also contain pyrimidine rings. In nucleic acids, three nucleobases are pyrimidine derivatives: cytosine, thymine and uracil. There are a variety of pyrimidine-containing drugs on the market, most of which are kinase inhibitors.
Scorpion presented initial, first-in-human clinical results from its Phase 1/2 study of STX-478 in advanced solid tumor patients in a Proffered Paper late-breaking session at the European Society for Medical Oncology (ESMO) Congress 2024 in Barcelona, Spain. Initial Phase 1 monotherapy data for STX-478, an oral, once-daily, mutant-selective, allosteric PI3Kα inhibitor, demonstrated potentially best-in-class PI3Kα inhibition, with anti-tumor activity observed in multiple cancer types, including HR+/HER2- breast cancer (BC), gynecological tumors, and other solid tumors. STX-478 was well-tolerated, including in pre-diabetic, diabetic and heavily pre-treated patients and showed no significant wild-type-mediated toxicities. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.