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

Bioorg Med Chem Lett. 2019 Aug 1;29(15):1922-1927. doi: 10.1016/j.bmcl.2019.05.047. Epub 2019 May 24.


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.

Keywords: Bleomycin mimic; Folate conjugate; Folate receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Bleomycin / pharmacology
  • Bleomycin / therapeutic use*
  • Folic Acid / pharmacology
  • Folic Acid / therapeutic use*
  • Humans
  • Neoplasms / drug therapy*


  • Antineoplastic Agents
  • Bleomycin
  • Folic Acid