Synthesis and Kinase Inhibitory Potencies of Pyrazolo[3,4-g]isoquinolines.

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.

Citation

Mathilde Defois, Chloé Rémondin, Béatrice Josselin, Lionel Nauton, Vincent Théry, Fabrice Anizon, Sandrine Ruchaud, Francis Giraud, Pascale Moreau. Synthesis and Kinase Inhibitory Potencies of Pyrazolo[3,4-g]isoquinolines. Molecules (Basel, Switzerland). 2022 Aug 30;27(17)

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PMID: 36080340

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