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

Arjan Geersing, Reinder H. de Vries, Gerrit Jansen, Marianne G. Rots, Gerard Roelfes

Research output: Contribution to journalArticleAcademicpeer-review


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.
Original languageEnglish
Pages (from-to)1922-1927
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number15
Publication statusPublished - 1 Aug 2019

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