0

Novel Meriolin Derivatives as Rapid Apoptosis Inducers

Daniel Drießen, Fabian Stuhldreier, Annika Frank, Holger Stark, Sebastian Wesselborg, Björn Stork, Thomas J J Müller

Bioorg Med Chem. 2019 Aug 1;27(15):3463-3468.

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
IAR42417812 Meriolin 2 Meriolin 2 Price
qrcode