Synthesis of new pyrazolo[4,3-a]phenanthridine Pim-1 inhibitors and evaluation of their cytotoxic activity towards the MOLM-13 acute myeloid leukemia cell line - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2022

Synthesis of new pyrazolo[4,3-a]phenanthridine Pim-1 inhibitors and evaluation of their cytotoxic activity towards the MOLM-13 acute myeloid leukemia cell line

Résumé

We synthesized new analogues of the anti-AML agent VS-II-173. We studied the effect of the substitution at the 1-and 5-positions of the pyrazolo[4,3-a]phenanthridine scaffold on Pim-1 kinase inhibition and cytotoxicity against AML MOLM-13 cells. We found that compounds 20 and 21, substituted at the 1-position exhibited stronger Pim-1 inhibition together with a high potency toward MOLM-13 cells, associated with apoptosis induction and selectivity over non-cancerous NRK cells.
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Dates et versions

hal-03764764 , version 1 (30-08-2022)

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Etienne Auvert, Reidun Aesoy, Francis Giraud, Lars Herfindal, Fabrice Anizon, et al.. Synthesis of new pyrazolo[4,3-a]phenanthridine Pim-1 inhibitors and evaluation of their cytotoxic activity towards the MOLM-13 acute myeloid leukemia cell line. Bioorganic and Medicinal Chemistry Letters, 2022, 73, pp.128914. ⟨10.1016/j.bmcl.2022.128914⟩. ⟨hal-03764764⟩
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