Novel meriolin derivatives as rapid apoptosis inducers.

Basic Information

ID: ALA4346731

Journal: Bioorg Med Chem

Title: Novel meriolin derivatives as rapid apoptosis inducers.

Authors: Drießen D, Stuhldreier F, Frank A, Stark H, Wesselborg S, Stork B, Müller TJJ.

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.

CiteXplore: 31248707

DOI: 10.1016/j.bmc.2019.06.029

Patent ID: