Synthesis and biological evaluation of 17(3)-dicarboxylethyl-pyropheophorbide-a amide derivatives for photodynamic therapy

Three novel 17(3)-dicarboxylethyl-pyropheophorbide-a amide derivatives as photosensitizers for photodynamic therapy (PDT) were synthesized from pyropheophorbide-a (Ppa). Their photophysical and photochemical properties, intracellular localization, photocytotoxicity in vitro and in vivo were investig...

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Published inBioorganic & medicinal chemistry letters Vol. 28; no. 16; pp. 2784 - 2788
Main Authors Zhu, Wei, Wang, Lai-Xing, Chen, Dan-Ye, Gao, Ying-Hua, Yan, Yi-Jia, Wu, Xiao-Feng, Wang, Mi, Han, Yi-Ping, Chen, Zhi-Long
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier 01.09.2018
Subjects
Chemistry
Chemistry, Medicinal
Chemistry, Organic
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
Chlorin
Chlorophyll
ACID-DERIVATIVES
IN-VITRO
Photodynamic therapy
BACTERIOPURPURINIMIDES
ANALOGS
POTENT PHOTOSENSITIZERS
Tumor
AGENTS
PHOTOPHYSICAL PROPERTIES
Photosensitizer
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Summary:Three novel 17(3)-dicarboxylethyl-pyropheophorbide-a amide derivatives as photosensitizers for photodynamic therapy (PDT) were synthesized from pyropheophorbide-a (Ppa). Their photophysical and photochemical properties, intracellular localization, photocytotoxicity in vitro and in vivo were investigated. All target compounds exhibited low cytotoxicity in the dark and remarkable photocytotoxicity against human esophageal cancer cells. Among them, la showed highest singlet oxygen quantum yield. Upon light activation, la exhibited significant photocytotoxicity. After PDT treatment, the growth of Eca-109 tumor in nude mice was significantly inhibited. Therefore, la is a powerful and promising antitumor photosensitizer for PDT. (C) 2017 Elsevier Ltd. All rights reserved.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2017.12.034