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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Geersing A,de Vries RH,Jansen G,Rots MG,Roelfes G

doi

10.1016/j.bmcl.2019.05.047

subject

Has Abstract

pub_date

2019-08-01 00:00:00

pages

1922-1927

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(19)30344-0

journal_volume

29

pub_type

杂志文章

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