Folic acid conjugates of a bleomycin mimic for selective targeting of folate receptor positive cancer cells.

Basic Information

ID: ALA4433233

Journal: Bioorg Med Chem Lett

Title: Folic acid conjugates of a bleomycin mimic for selective targeting of folate receptor positive cancer cells.

Authors: Geersing A, de Vries RH, Jansen G, Rots MG, Roelfes G.

Abstract: A major challenge in the application of cytotoxic anti-cancer drugs is their general lack of selectivity, which often leads to systematic toxicity due to their inability to discriminate between malignant and healthy cells. A particularly promising target for selective targeting are the folate receptors (FR) that are often over-expressed on cancer cells. Here, we report on a conjugate of the pentadentate nitrogen ligand N4Py to folic acid, via a cleavable disulphide linker, which shows selective cytotoxicity against folate receptor expressing cancer cells.

CiteXplore: 31155430

DOI: 10.1016/j.bmcl.2019.05.047

Patent ID: