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

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Suzuki T,Hisakawa S,Itoh Y,Suzuki N,Takahashi K,Kawahata M,Yamaguchi K,Nakagawa H,Miyata N

doi

10.1016/j.bmcl.2007.05.040

subject

Has Abstract

pub_date

2007-08-01 00:00:00

pages

4208-12

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)00593-8

journal_volume

17

pub_type

杂志文章

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