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Novel meriolin derivatives as rapid apoptosis inducers.

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Affiliations

  • 1. Institut für Organische Chemie und Makromolekulare Chemie, Heinrich-Heine-Universität Düsseldorf, Universitätsstraße 1, D-40225 Düsseldorf, Germany.
      Authors
    • Drießen D 1
    • Müller TJJ 1
    (2 authors)
  • 2. Institut für Molekulare Medizin I, Heinrich-Heine-Universität Düsseldorf, Universitätsstraße 1, D-40225 Düsseldorf, Germany.
      Authors
    • Stuhldreier F 2
    • Wesselborg S 2
    • Stork B 2
    (3 authors)
  • 3. Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf, Universitätsstraße1, D-40225 Düsseldorf, Germany.
      Authors
    • Frank A 3
    • Stark H 3
    (2 authors)

ORCIDs linked to this article

Bioorganic & Medicinal Chemistry, 19 Jun 2019, 27(15):3463-3468
https://doi.org/10.1016/j.bmc.2019.06.029 PMID: 31248707 

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.

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