公开(公告)号：EP4316476A1

公开(公告)日：2024-02-07

申请号：EP22386055.2

申请日：2022-08-02

申请人： University of Crete ,  National and Kapodistrian University of Athens ,  Elipoulos, G. Aristides

发明人： Vassilikogiannakis, Georgios ,  Eliopoulos, G. Aristides ,  Stratakis, Manolis ,  Montagnon, Tamsyn ,  Kalaitzakis, Dimitris

IPC分类号： A61K31/122 ,  A61K31/69 ,  A61P35/00

摘要： The invention discloses novel 4-hydroxycyclopent-2-en-1-one derivatives as active compounds in pharmaceutical compositions for the treatment of cancer. The invention confers cytotoxic effects of the said compounds on ovarian, colorectal, cervical, hepatocellular, lung, bladder and breast carcinomas, melanoma, lymphoma and myeloma malignant cells, for the inhibition of cell cycle progression at the G2/M phase, for reducing the expression of DNA replication licensing factors and for having general cancer treatment effects. It further discloses the use of the said compositions for the treatment of platinum-resistant tumors. Another aspect of the invention is the synergetic effects of these compounds with existing cancer treatment medicaments as the proteasomal inhibitors. Finally, the synthetic methods of the active compounds of the said compositions are disclosed.