Design, synthesis, and biological activity of folate receptor-targeted prodrugs of thiolate histone deacetylase inhibitors

Autor:	Shinya Hisakawa, Hidehiko Nakagawa, Takayoshi Suzuki, Katsumasa Takahashi, Kentaro Yamaguchi, Yukihiro Itoh, Masatoshi Kawahata, Naoki Miyata, Nobuaki Suzuki
Rok vydání:	2007
Předmět:	medicine.drug_class Clinical Biochemistry Pharmaceutical Science Receptors Cell Surface Biochemistry Cell Line Tumor Drug Discovery medicine Humans Prodrugs Sulfhydryl Compounds Enzyme Inhibitors Molecular Biology Vorinostat chemistry.chemical_classification biology Organic Chemistry Histone deacetylase inhibitor Folate Receptors GPI-Anchored Biological activity Prodrug Histone Deacetylase Inhibitors Enzyme chemistry Folate receptor Enzyme inhibitor Drug Design biology.protein Molecular Medicine Histone deacetylase Carrier Proteins medicine.drug
Zdroj:	Bioorganicmedicinal chemistry letters. 17(15)
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ded1087cdc337196755b2dde299a3b7c https://pubmed.ncbi.nlm.nih.gov/17532630 Zobrazit plný text záznamu Full Text from ScienceDirect