摘要

A series of 1,4-naphthoquinones (10a-10q) were synthesized and evaluated for anticancer activity. Compound 10e was identified as an inhibitor of Itch, a HECT domain-E3 ligase. In an evaluation of in vivo efficacy, 10e exhibited remarkable anticancer activity with TGI values of 98.3% and 100% at 25 mg/kg and 50 mg/kg orally daily, respectively, against human RPMI-8226 multiple myeloma xenograft. Treatment with 10e also showed a decrease of Itch level in human RPMI-8226 multiple myeloma cells. Thus 10e is a lead compound for further development of inhibitors targeting E3 ligase for treatment of multiple myeloma.
原文英語
頁(從 - 到)84-91
頁數8
期刊European Journal of Medicinal Chemistry
140
DOIs
出版狀態已發佈 - 十一月 10 2017

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

指紋 深入研究「1,4-Naphthoquinones as inhibitors of Itch, a HECT domain-E3 ligase, and tumor growth suppressors in multiple myeloma」主題。共同形成了獨特的指紋。

引用此