Anticancer and Structure Activity Relationship of Non-Symmetrical Choline Kinase Inhibitors.

ABSTRACT: Choline kinase inhibitors are an outstanding class of cytotoxic compounds useful for the treatment of different forms of cancer since aberrant choline metabolism is a feature of neoplastic cells. Here, we present the most in-depth structure-activity relationship studies of an interesting series of non-symmetric choline kinase inhibitors previously reported by our group: 3a-h and 4a-h. They are characterized by cationic heads of 3-aminophenol bound to 4-(dimethylamino)- or 4-(pyrrolidin-1-yl)pyridinium through several linkers. These derivatives were evaluated both for their inhibitory activity on the enzyme and their antiproliferative activity in a panel of six human tumor cell lines. The compounds with the N-atom connected to the linker (4a-h) show

SUBMITTER: Schiaffino-Ortega S 

PROVIDER: S-EPMC8464809 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature