Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 15, Pages 4208-4212Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.05.040
Keywords
histone deacetylase inhibitor; selective anticancer activity; folate conjugate; prodrug
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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 I was significantly reduced by free folic acid, suggesting that cellular uptake of I is mediated by FR. (c) 2007 Elsevier Ltd. All rights reserved.
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