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Synthesis and biological studies of the thiols-triggered anticancer prodrug for a more effective cancer therapy.

Abstract
A novel anticancer prodrug compound 1, which was designed to be triggered by thiols and release the chemotherapeutic agent mechlorethamine, was successfully prepared and evaluated for the first time. The activation of compound 1 was determined by NMR analysis and denaturing alkaline agarose gel electrophoresis. A fluorescence image and comet assay indicated that the inducible reactivity of 1 could be accomplished in cell media. The anticancer activities are also discussed.
AuthorsYuanzhen Xu, Jianjun Chen, Ya Li, Shoujiao Peng, Xueyan Gu, Meng Sun, Kun Gao, Jianguo Fang
JournalOrganic & biomolecular chemistry (Org Biomol Chem) Vol. 13 Issue 9 Pg. 2634-9 (Mar 07 2015) ISSN: 1477-0539 [Electronic] England
PMID25581090 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Prodrugs
  • Sulfhydryl Compounds
  • Mechlorethamine
Topics
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Mechlorethamine (chemical synthesis, chemistry, pharmacology)
  • Molecular Structure
  • Prodrugs (chemical synthesis, chemistry, pharmacology)
  • Structure-Activity Relationship
  • Sulfhydryl Compounds (chemical synthesis, chemistry, pharmacology)

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