Article
Modification of a promiscuous inhibitor shifts the inhibition from γ-secretase to FLT-3.
Bioorganic & medicinal chemistry letters - 15 Dec 2012
Amombo Ghislaine Marlyse Okala, Kramer Thomas, Lo Monte Fabio, Göring Stefan, Fach Matthias, Smith Steven, Kolb Stephanie, Schubenel Robert, Baumann Karlheinz, Schmidt Boris
Abstract excerpt
The inhibition of FLT-3 activity is an interesting target for the treatment of acute myeloid leukemia (AML). The serendipitous identification of FLT-3 inhibitors from a CK1/γ-secretase programme provided compounds with dual inhibitory activity. We analyzed the structure-activity relationship of these inhibitors and derivatized them to arrive at compounds with reduced impact on γ-secretase activity and enhanced...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.