1415609-38-9Relevant academic research and scientific papers
Modification of a promiscuous inhibitor shifts the inhibition from γ-secretase to FLT-3
Amombo, Ghislaine Marlyse Okala,Kramer, Thomas,Lo Monte, Fabio,Goering, Stefan,Fach, Matthias,Smith, Steven,Kolb, Stephanie,Schubenel, Robert,Baumann, Karlheinz,Schmidt, Boris
supporting information, p. 7634 - 7640 (2013/02/21)
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 FLT-3 inhibition.
