Hélène Losson Gajulapalli, Sruthi Reddy Manon Lernoux Lee, Jin-Young Mazumder, Aloran Gérard, Déborah Seidel Carole Hahn, Hyunggu Christov, Christo Dicato, Mario
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Published in
Pharmacological Research
Despite the discovery of tyrosine kinase inhibitors (TKIs) for the treatment of breakpoint cluster region-Abelson (BCR-ABL) + cancer types, patients with chronic myeloid leukemia (CML) treated with TKIs develop resistance and severe adverse effects. Combination treatment, especially with a histone deacetylase (HDAC) 6 inhibitor (HDAC6i), appears to...
Manon Lernoux Michael Schnekenburger Hélène Losson Vermeulen, Koen Hahn, Hyunggu Gérard, Déborah Lee, Jin-Young Mazumder, Aloran Ahamed, Muneer Christov, Christo
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Published in
Clinical Epigenetics
Background: Chronic myeloid leukemia (CML) pathogenesis is mainly driven by the oncogenic breakpoint cluster region-Abelson murine leukemia viral oncogene homolog 1 (BCR-ABL) fusion protein. Since BCR-ABL displays abnormal constitutive tyrosine kinase activity, therapies using tyrosine kinase inhibitors (TKis) such as imatinib represent a major bre...
Michael Schnekenburger Goffin, Eric Lee, Jin-Young Young Jang, Jun Mazumder, Aloran Ji, Seungwon Rogister, Bernard Bouider, Nafila Lefranc, Florence Miklos, Walter
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Published in
Journal of Medicinal Chemistry
A new series of N-aryl-N'-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)ureas bearing an alkoxycarbonylamino group at the 6-position were synthesized and examined as putative anticancer agents targeting sirtuins in glioma cells. Based on computational docking combined to in vitro sirtuin 1/2 inhibition assays, we selected compound 18 [R/S-N-3-cyano...