A thiol-inducible and quick-response DNA cross-linking agent |
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| Authors: | Yuanzhen Xu Hongbo Wei Jianjun Chen Kun Gao |
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| Institution: | 1. State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Gansu, Lanzhou 730000, China;2. Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Shaanxi, Yangling 712100, China |
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| Abstract: | Three new 2,4-dinitrobenzenesulfonyl derivatives 1–3 were successfully prepared for the first time using a simple process. They were efficiently triggered by thiols (glutathione and l-cysteine) to release the corresponding phenol derivatives (4–6) within 5?min. The quick response of 1–3 toward thiols was determined by 1H NMR and HPLC. Moreover, our results indicated that 1 could induce DNA cross-linking in the presence of glutathione, probably due to the quinone methide formation of phenol intermediate 4 followed by departure of 2,4-dinitrobenzenesulfonyl group. |
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| Keywords: | Quinone methide DNA cross-linking Antitumor agents 2 4-Dinitrobenzenesulfonyl |
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