Short oligonucleotide prodrug having 5-fluoro and 5-iodouracil inhibits the proliferation of cancer cells in a photo-responsive manner.

Authors :: Fujimoto K
Takematsu YK
Shigeno A
Furusawa M
Sakamoto T
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2014 Aug 15; Vol. 24 (16), pp. 3736-8. Date of Electronic Publication: 2014 Jul 14.
Publication Year :: 2014
Abstract: Photo-induced C1' hydrogen abstraction of 5-fluoro-2'-deoxyuridine was adopted as the key reaction for releasing 5-fluorouracil (5-FU) anticancer drug from oligonucleotide strands. After photoirradiation following 5-FU release, anticancer activity was expected. We demonstrated that oligonucleotide tetramer, d(A(F)U(I)UA), can release 5-FU under physiological conditions in a photo-responsive manner thorough photo-induced C1' hydrogen abstraction, and that the 5-FU released from d(A(F)U(I)UA) having a phosphorothioate backbone clearly suppresses the proliferation of HeLa cells in a photo-responsive manner.<br /> (Copyright © 2014 Elsevier Ltd. All rights reserved.)

Full Text Access

Tools