Recent developments in Haspin kinase inhibitors: Structure, synthesis and activities

Haspin is an atypical serine/threonine protein kinase involved in the regulation of mitosis progression. In the recent years, significant progress, especially in terms of selectivity, has been achieved in the discovery of Haspin inhibitors. Based on Haspin structure knowledge, rational design identified various chemical series such as indole, indazole, quinoline, isoquinoline, benzothiophene and purine derivatives exhibiting potent Haspin inhibitory activity and good selectivity profiles when tested toward large kinase panels. In this review, we present recent findings on Haspin inhibitors, classified by chemical family, reported in the patented and journal literature since 2022.