Abstract
L-Cysteine (Cys)-activatable photosensitizer 3 was designed and synthesized based on hypocrellin B (1). Cys is a novel tumor-associated biomarker. 3 exhibited negligible photosensitizing ability without Cys. However, when 1 was released from 3 by reaction with Cys, the photosensitizing activity was restored. Furthermore, 3 showed selective and effective photo-cytotoxicity against only cancer cells such as HeLa and A549 cells that highly express Cys when irradiated with 660 nm light, which is inside the phototherapeutic window.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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A549 Cells
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Antineoplastic Agents* / chemical synthesis
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Antineoplastic Agents* / chemistry
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Antineoplastic Agents* / pharmacology
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Cell Survival / drug effects
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Cysteine* / chemistry
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Drug Screening Assays, Antitumor
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HeLa Cells
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Humans
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Molecular Structure
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Perylene* / analogs & derivatives
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Perylene* / chemical synthesis
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Perylene* / chemistry
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Perylene* / pharmacology
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Photochemotherapy
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Photosensitizing Agents* / chemical synthesis
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Photosensitizing Agents* / chemistry
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Photosensitizing Agents* / pharmacology
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Quinones* / chemical synthesis
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Quinones* / chemistry
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Quinones* / pharmacology
Substances
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Quinones
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Photosensitizing Agents
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Perylene
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hypocrellin B
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Cysteine
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Antineoplastic Agents