Design, Synthesis, and Biological Activity of Releasable m-THPC-PEGfolate Conjugate Using a Disulfide-containing Linker
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Published:2019-02-11
Issue:3
Volume:16
Page:165-169
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ISSN:1570-1786
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Container-title:Letters in Organic Chemistry
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language:en
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Short-container-title:LOC
Author:
Xi Li Peng1, Hong Li Dong2, Chuan Wan1, Shou Chen Ben1
Affiliation:
1. Chongqing Chemical Industry Vocational College, Chongqing 400020, China 2. State Key Laboratory of Trauma, Burn and Combined Injury, The 2nd Department of Research Institute of Surgery, Third Military Medical University, Chongqing 400042, China
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.
Publisher
Bentham Science Publishers Ltd.
Subject
Organic Chemistry,Biochemistry
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