pyrazolo[3,4-d]pyrimidine SRC inhibitor

Pyrazolo[3,4-d]pyrimidine SRC inhibitors represent a class of small-molecule, ATP-competitive tyrosine kinase inhibitors (TKIs) specifically designed to target the Src family of non-receptor tyrosine kinases (SFKs). This chemical scaffold was primarily developed through academic research collaborations between the University of Genova and the University of Siena, with support from Lead Discovery Siena S.r.L. These compounds, which include research candidates like Si306 and its prodrug form pro-Si306, inhibit c-Src and related kinases such as Fyn and Bcr-Abl, which are frequently overexpressed or overactive in various malignancies. Preclinical studies have highlighted their potential in treating highly invasive cancers, particularly glioblastoma, where they have shown the ability to cross the blood-brain barrier and reduce tumor cell migration and invasion. Other investigated indications include medulloblastoma and prostate cancer.