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Article Dans Une Revue Bioorganic and Medicinal Chemistry Année : 2024

Synthesis and biological evaluation of 1H-pyrrolo[3,2–g]isoquinolines

Résumé

A structure-activity relationship study performed on 1H-pyrrolo[3,2-g]isoquinoline scaffold identified new haspin inhibitors with nanomolar potencies and selectivity indices (SI) over 6 (inhibitory potency evaluated against 8 protein kinases). Compound 22 was the most active of the series (haspin IC50 = 76 nM). Cellular evaluation of 22 confirmed its activity for endogenous haspin in U-2 OS cells and its anti-proliferative activity against various cell lines. In addition, the binding mode of analog 22 in complex with haspin was determined by X-ray crystallography.
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hal-04441218 , version 1 (06-02-2024)

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Mathilde Defois, Béatrice Josselin, Pierre Brindeau, Andreas Krämer, Stefan Knapp, et al.. Synthesis and biological evaluation of 1H-pyrrolo[3,2–g]isoquinolines. Bioorganic and Medicinal Chemistry, 2024, 100, pp.117619. ⟨10.1016/j.bmc.2024.117619⟩. ⟨hal-04441218⟩
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