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

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 kina...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-01, Vol.23 (1), p.117-118
Hauptverfasser:	Takahashi, Yohei, Kubota, Takaaki, Yamamoto, Sunao, Kobayashi, Jun’ichi
Format:	Artikel
Sprache:	eng
Schlagworte:	Cell Line, Tumor Cell Survival - drug effects chemistry EGFR HER2 Humans Marine sponge Metachromins phosphotransferases (kinases) Porifera Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - toxicity quinones Receptor, Epidermal Growth Factor - antagonists & inhibitors Receptor, Epidermal Growth Factor - metabolism Receptor, ErbB-2 - antagonists & inhibitors Receptor, ErbB-2 - metabolism Sesquiterpenes - chemical synthesis Sesquiterpenes - chemistry Sesquiterpenes - toxicity Spongia sp Structure-Activity Relationship tyrosine
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Beschreibung
Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.11.001