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

吡唑并[3,4-g]异喹啉的合成及激酶抑制活性

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作者:Mathilde Defois, Chloé Rémondin, Béatrice Josselin, Lionel Nauton, Vincent Théry, Fabrice Anizon, Sandrine Ruchaud, Francis Giraud, Pascale Moreau

Abstract

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.

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