Inhibitory effects of metachromins L-Q and its related analogs against receptor tyrosine kinases EGFR and HER2

Yohei Takahashi; Takaaki Kubota; Sunao Yamamoto; Jun'ichi Kobayashi

doi:10.1016/j.bmcl.2012.11.001

Inhibitory effects of metachromins L-Q and its related analogs against receptor tyrosine kinases EGFR and HER2

Bioorg Med Chem Lett. 2013 Jan 1;23(1):117-8. doi: 10.1016/j.bmcl.2012.11.001. Epub 2012 Nov 10.

Authors

Yohei Takahashi¹, Takaaki Kubota, Sunao Yamamoto, Jun'ichi Kobayashi

Affiliation

¹ Graduate School of Pharmaceutical Sciences, Hokkaido University, Sapporo 060-0812, Japan.

PMID: 23219324
DOI: 10.1016/j.bmcl.2012.11.001

Abstract

Metachromins are a series of sesquiterpenoid quinones isolated from Okinawan marine sponges. Inhibitory effects of metachromins L-Q (1-6), sesquiterpenoid quinones with an amino acid residue, and their related analogs (7-18) prepared from metachromins A (19) and C (20) against receptor tyrosine kinases EGFR and HER2 were investigated. Two analogs 11 and 12 showed relatively stronger inhibitory activity against EGFR, while metachromins L-Q (1-6) and seven analogs (8, 10, 11, and 15-18) showed inhibitory activities against HER2.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Cell Line, Tumor
Cell Survival / drug effects
ErbB Receptors / antagonists & inhibitors*
ErbB Receptors / metabolism
Humans
Protein Kinase Inhibitors / chemical synthesis
Protein Kinase Inhibitors / chemistry*
Protein Kinase Inhibitors / toxicity
Receptor, ErbB-2 / antagonists & inhibitors*
Receptor, ErbB-2 / metabolism
Sesquiterpenes / chemical synthesis
Sesquiterpenes / chemistry*
Sesquiterpenes / toxicity
Structure-Activity Relationship

Substances

Protein Kinase Inhibitors
Sesquiterpenes
ErbB Receptors
Receptor, ErbB-2