title: 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.
authors.affiliation: State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, PR China. npchem@lzu.edu.cn.
authors.forename: Yuanzhen
authors.initials: Y
authors.lastname: Xu
authors.forename: Jianjun
authors.initials: J
authors.lastname: Chen
authors.forename: Ya
authors.initials: Y
authors.lastname: Li
authors.forename: Shoujiao
authors.initials: S
authors.lastname: Peng
authors.forename: Xueyan
authors.initials: X
authors.lastname: Gu
authors.forename: Meng
authors.initials: M
authors.lastname: Sun
authors.forename: Kun
authors.initials: K
authors.lastname: Gao
authors.forename: Jianguo
authors.initials: J
authors.lastname: Fang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008466:Mechlorethamine / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D011355:Prodrugs / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D011355:Prodrugs; D013438:Sulfhydryl Compounds; D008466:Mechlorethamine