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Novel meriolin derivatives as rapid apoptosis inducers |
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| Authors: | Daniel Drießen Fabian Stuhldreier Annika Frank Holger Stark Sebastian Wesselborg Björn Stork Thomas J.J. Müller |
| Affiliation: | 1. Institut für Organische Chemie und Makromolekulare Chemie, Heinrich-Heine-Universität Düsseldorf, Universitätsstraße 1, D-40225 Düsseldorf, Germany;2. Institut für Molekulare Medizin I, Heinrich-Heine-Universität Düsseldorf, Universitätsstraße 1, D-40225 Düsseldorf, Germany;3. Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf, Universitätsstraße1, D-40225 Düsseldorf, Germany |
| Abstract: | 3-(Hetero)aryl substituted 7-azaindoles possessing multikinase inhibitor activity are readily accessed in a one-pot Masuda borylation-Suzuki coupling sequence. Several promising derivatives were identified as apoptosis inducers and, emphasizing the multikinase inhibition potential, as sphingosine kinase 2 inhibitors. Our measurements provide additional insights into the structure-activity relationship of meriolin derivatives, suggesting derivatives bearing a pyridine moiety with amino groups in 2-position as most active anticancer compounds and thus as highly promising candidates for future in vivo studies. |
| Keywords: | Corresponding author. Synthetic methods One-pot reaction Masuda borylation-Suzuki coupling Meriolin Apoptosis Sphingosine kinase 2 |
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