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A highly GSH-sensitive SN-38 prodrug with an "OFF-to-ON" fluorescence switch as a bifunctional anticancer agent
- Authors
- 김경수; Yoo, E (Yoo, Eunsoo); Kim, D (Kim, Dongin); Whang, CH (Whang, Chang-Hee); Jo, S (Jo, Seongbong); Hur, SK (Hur, Seong Kwon)
- Issue Date
- Jul-2018
- Publisher
- ROYAL SOC CHEMISTRY
- Citation
- CHEMICAL COMMUNICATIONS, v.54, no.65, pp 9031 - 9034
- Pages
- 4
- Indexed
- SCI
SCIE
SCOPUS
- Journal Title
- CHEMICAL COMMUNICATIONS
- Volume
- 54
- Number
- 65
- Start Page
- 9031
- End Page
- 9034
- ISSN
- 1359-7345
1364-548X
- Abstract
- SN-38 (7-ethyl-10-hydroxy-camptothecin) is an active metabolite of irinotecan (CPT-11) and the most potent camptothecin analogue. In this study, 2,4-dinitrobenzene sulfonyl (DNS) was covalently conjugated as a GSH-sensitive trigger to 10' -OH of SN-38 to yield a GSH-sensitive prodrug, denoted as DNS-SN38, with virtually quenched fluorescence due to donor-excited photo-induced electron transfer (d-PeT). By investigating DNS-SN38's activation properties upon fluorescence restoration and cytotoxic potency against ovarian cancer cell lines (A2780 and m-Cherry + OCSC1-F2), its potential applicability as a useful chemotherapeutic agent was demonstrated.
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