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Letters in Organic Chemistry

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ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

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Letter Article

Design, Synthesis, and Biological Activity of Releasable m-THPC-PEGfolate Conjugate Using a Disulfide-containing Linker

Author(s): Li Peng Xi*, Li Dong Hong, Wan Chuan and Chen Ben Shou

Volume 16, Issue 3, 2019

Page: [165 - 169] Pages: 5

DOI: 10.2174/1570178615666181003124619

Price: $65

Abstract

The present study reported the preparation of a novel mutual prodrug containing meso-tetra (m-hydroxy phenyl) chlorin (m-THPC), PEG and folate. The folate receptor (FR) targeting compound is a water-soluble chemical incorporating a hydrophilic PEG spacer unit and a reducible selfimmolative disulfide-based linker system between the FR-targeting ligand and the chlorin. The m- THPC-s-s-PEG-Folate was proved to release the parent drug and exhibited significant targeting effects on HeLa cells. In addition, the redox-responsive folate targeting photosensitizer m-THPC-s-s-PEG-Folate showed slightly higher phototoxicity than m-THPC-PEG-Folate for HeLa cells.

Keywords: m-THPC, folate, disulfide, tumor, PEG, releasable.

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