Nanjing China-Australia Institute of Translational Medicine Co.Ltd.
发明人:
Quan ZHAO,Renxiang TAN,Yadong WANG,Liping LIN
申请号：
US16408549
公开号：
US20200031807A1
申请日:
2019.05.10
申请国别(地区):
US
年份:
2020
代理人:
摘要：
Disclosed are a small-molecule AURKB inhibitor and applications thereof. The invention is directed to a diindolylmethane compound of formula (I) or a stereoisomer, a tautomer, a solvate, a prodrug, a N-oxide or a pharmaceutically acceptable salt thereof. The invention also provides an application of the small-molecule inhibitor and a modified derivative thereof (such as a stereoisomer, a tautomer, a solvate, a prodrug, an N-oxide or a pharmaceutically acceptable salt) in the preparation of an antitumor drug. The small-molecule AURKB inhibitor identified herein is slightly toxic to those normal cells and can significantly inhibit the expression of a downstream gene E2F2 mediated in the phosphorylation of an AURKB substrate histone H3S10. Therefore, the small-molecule inhibitor, as an anti-tumor drug, can effectively inhibit the proliferation of various tumor cells and induce the apoptosis of tumor cells.
