公开(公告)号：US11780833B2

公开(公告)日：2023-10-10

申请号：US16045254

申请日：2018-07-25

Applicant: HOWARD UNIVERSITY

Inventor： Oladapo Bakare ,  Samuel Ray Denmeade ,  Emmanuel S. Akinboye

IPC: C07K7/06 ,  C07D455/08 ,  C07D401/06

CPC classification number: C07D455/08 ,  C07D401/06 ,  C07K7/06

Abstract: Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2′-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia.