Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1366204 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Aiming to develop selective anticancer drugs, we designed and synthesized three disulfides bearing a folic acid moiety as candidate folate receptor (FR)-targeted prodrugs of thiolate histone deacetylase inhibitors. Among them, compound 1 displayed growth-inhibitory activity toward folate receptor-positive MCF-7 breast cancer cells. The activity of 1 was significantly reduced by free folic acid, suggesting that cellular uptake of 1 is mediated by FR.
Graphical abstractAiming to develop selective anticancer drugs, we designed and synthesized three disulfides bearing a folic acid moiety as candidate folate receptor (FR)-targeted prodrugs of thiolate histone deacetylase inhibitors. One of the folate conjugates showed growth-inhibitory activity toward folate receptor-positive MCF-7 breast cancer cells.Figure optionsDownload full-size imageDownload as PowerPoint slide