title: Synthesis and cytotoxicity of novel artemisinin derivatives containing sulfur atoms.
abstract: Ten novel artemisinin derivatives containing sulfur atoms were designed and synthesized and their structures were confirmed by (1)H NMR, (13)C NMR and HRMS technologies in this study. All compounds were reported for the first time. The in vitro cytotoxicity against PC-3, SGC-7901, A549 and MDA-MB-435s cancer cell lines was evaluated by MTT assay. Compounds 4a and 4f displayed potent antitumor activity against PC-3, SGC-7901 and A549 cells with IC50 ranging from 1.6 to 30.5 μM, which values are compared to that of 5-FU (IC50 from 6.8 to 42.5 μM). Compounds 4a and 4f showed high specificity towards human lung cancer A549 cells compared to normal human hepatic L-02 cells with selectivity index of 16.1 and 50.1 respectively. Our promising findings indicated that the compounds 4a and 4f could stand as potential lead compounds for further investigation.
authors.affiliation: Jiangsu Key Laboratory of TCM Evaluation and Translational Research, China Pharmaceutical University, Nanjing, Jiangsu 211198, China.
authors.forename: Cang-Cang
authors.initials: CC
authors.lastname: Xu
authors.affiliation: Jiangsu Key Laboratory of TCM Evaluation and Translational Research, China Pharmaceutical University, Nanjing, Jiangsu 211198, China.
authors.forename: Juan-Juan
authors.initials: JJ
authors.lastname: Wu
authors.affiliation: Jiangsu Key Laboratory of TCM Evaluation and Translational Research, China Pharmaceutical University, Nanjing, Jiangsu 211198, China.
authors.forename: Tao
authors.initials: T
authors.lastname: Xu
authors.affiliation: Jiangsu Key Laboratory of TCM Evaluation and Translational Research, China Pharmaceutical University, Nanjing, Jiangsu 211198, China.
authors.forename: Chun-Hua
authors.initials: CH
authors.lastname: Yao
authors.affiliation: Jiangsu Key Laboratory of TCM Evaluation and Translational Research, China Pharmaceutical University, Nanjing, Jiangsu 211198, China; State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu 210009, China. Electronic address: boyangyu59@163.com.
authors.forename: Bo-Yang
authors.initials: BY
authors.lastname: Yu
authors.affiliation: Jiangsu Key Laboratory of TCM Evaluation and Translational Research, China Pharmaceutical University, Nanjing, Jiangsu 211198, China. Electronic address: liujihua@cpu.edu.cn.
authors.forename: Ji-Hua
authors.initials: JH
authors.lastname: Liu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D037621:Artemisinins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D060326:Chemistry Techniques, Synthetic; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D013329:Structure-Activity Relationship; D013455:Sulfur / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D037621:Artemisinins; D013455:Sulfur; C031327:artemisinin
keywords: Cytotoxicity; Novel artemisinin derivatives; Synthesis