Afficher la couverture '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 | Auvert, Etienne' en grand format
/5

0 avis

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

Auvert, Etienne | Aesoy, Reidun | Giraud, Francis | Herfindal, Lars | Anizon, Fabrice | Moreau, Pascale

Edité par CCSD ; Elsevier -

International audience. 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.

Suggestions

Du même auteur

Synthesis, kinase inhibition and anti-leukemic activities of diversely substituted indolopyrazolocarbazoles

Archive ouverte | Frazier, Théo | CCSD

International audience. Pyrazole analogues of the staurosporine aglycone K252c, in which the lactam ring was replaced by a pyrazole moiety, were synthesized. In this series, one or the other nitrogen atoms of the in...

A Kinase Inhibitor with Anti-Pim Kinase Activity is a Potent and Selective Cytotoxic Agent Toward Acute Myeloid Leukemia

Archive ouverte | Bjørnstad, Ronja | CCSD

International audience

Liposomes loaded with daunorubicin and an emetine prodrug for improved selective cytotoxicity towards acute myeloid leukaemia cells

Archive ouverte | Reiten, Ingeborg Nerbø | CCSD

International audience

Chargement des enrichissements...