Folic acid conjugates of a bleomycin mimic for selective targeting of folate receptor positive cancer cells. Issue 15 (1st August 2019)

• Record Type: Journal Article
• Authors: Geersing, Arjan; de Vries, Reinder H.; Jansen, Gerrit; Rots, Marianne G.; Roelfes, Gerard
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 29:Issue 15(2019)
• Page Start: 1922
• Page End: 1927
• Publication Date: 2019-08-01
• Subjects: Folate conjugate -- Bleomycin mimic -- Folate receptor; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2019.05.047
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.