Pyrazolopyrimidine scaffolds are one of the most important heterocyclic compounds in drug discovery. This scaffold has various biological activities, among which anticancer is an important one.
Wee1 protein is the most well-known Wee protein, and Wee1 protein kinases are members of the serine/threonine family and are highly conserved in evolution and are abundantly present in many eukaryotes and are very active in the S and G2 phases of the cell cycle. Wee1 protein kinase is a key regulatory center in DNA replication, chromosomal concentration, and histone transcription. These biological behavioral abnormalities can lead to genomic instability and cause malignant tumors, but inhibition or down-regulation of Wee1 protein kinase expression in malignant tumors can trigger mitotic catastrophe and apoptosis leads to tumor cell death. It has now been found that the expression of Wee1 is up-regulated in many cancers, and it has been clinically found that treatment with an inhibitor of Wee1 can effectively improve the occurrence and development of cancer. At present, many companies have deployed this target, and some have progressed to the clinical stage. Some Wee1 inhibitors under development include Adavosertib(ADZ1775), Azenosertib, ZNL-06-096, Debio-0123 and SGR-3515. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.
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