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Issue 65, 2018
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A highly GSH-sensitive SN-38 prodrug with an “OFF-to-ON” fluorescence switch as a bifunctional anticancer agent

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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.

Graphical abstract: A highly GSH-sensitive SN-38 prodrug with an “OFF-to-ON” fluorescence switch as a bifunctional anticancer agent

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Publication details

The article was received on 22 Jun 2018, accepted on 18 Jul 2018 and first published on 18 Jul 2018


Article type: Communication
DOI: 10.1039/C8CC05010D
Citation: Chem. Commun., 2018,54, 9031-9034
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    A highly GSH-sensitive SN-38 prodrug with an “OFF-to-ON” fluorescence switch as a bifunctional anticancer agent

    C. Whang, E. Yoo, S. K. Hur, K. S. Kim, D. Kim and S. Jo, Chem. Commun., 2018, 54, 9031
    DOI: 10.1039/C8CC05010D

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