Synthesis and biological activity of pyrazole analogues of the staurosporine aglycon K252c. - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Bioorganic and Medicinal Chemistry Année : 2016

Synthesis and biological activity of pyrazole analogues of the staurosporine aglycon K252c.

Résumé

A derivative of the staurosporine aglycon (K252c), in which the lactam ring was replaced by a pyrazole moiety, was synthesized. The resulting indolopyrazolocarbazole (3) inhibited Pim isoforms 1–3 whereas it did not impair the activity of two known targets of K252c, protein kinase C isoforms α and γ. Compound 3 exhibited moderate cytotoxic activity toward human leukemia and colon carcinoma cell lines (K562 and HCT116), strongly suggesting that this new scaffold deserves further investigations for treatment of malignancies associated with Pim activity.

Domaines

Chimie
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Dates et versions

hal-01367761 , version 1 (16-09-2016)

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Yannick J. Esvan, Francis Giraud, Elisabeth Pereira, Virginie Suchaud, Lionel Nauton, et al.. Synthesis and biological activity of pyrazole analogues of the staurosporine aglycon K252c. . Bioorganic and Medicinal Chemistry, 2016, 24, pp.3116-3124. ⟨10.1016/j.bmc.2016.05.032⟩. ⟨hal-01367761⟩
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