Sorbonne Université, CNRS, Plateforme de Criblage KISSf (Kinase Inhibitor Specialized Screening Facility), Protein Phosphorylation and Human Diseases Unit, Station Biologique, Place Georges Teissier, F-29688 Roscoff, France
A new series of pyrazolo[3,4-g]isoquinoline derivatives, diversely substituted at the 4- or 8-position, were synthesized. The results of the kinase inhibitory potency study demonstrated that the introduction of a bromine atom at the 8-position was detrimental to Haspin inhibition, while the introduction of an alkyl group at the 4-position led to a modification of the kinase inhibition profiles. Altogether, the results obtained demonstrated that new pyrazolo[3,4-g]isoquinolines represent a novel family of kinase inhibitors with various selectivity profiles.
