Modification of a promiscuous inhibitor shifts the inhibition from γ-secretase to FLT-3

…, S Kolb, R Schubenel, K Baumann, B Schmidt

文献索引：Amombo, Ghislaine Marlyse Okala; Kramer, Thomas; Lo Monte, Fabio; Goering, Stefan; Fach, Matthias; Smith, Steven; Kolb, Stephanie; Schubenel, Robert; Baumann, Karlheinz; Schmidt, Boris Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 24 p. 7634 - 7640

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被引用次数: 3

摘要

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.