title: Synthesis and Antitumor Activities of Chiral Dipeptide Thioureas Containing an Alpha-Aminophosphonate Moiety.
abstract: Thiourea derivatives demonstrate potent cytotoxic activity against various leukemias and many tumor cell lines. In our previous study, the combination of thiourea and phosphonate has been proven as an effective strategy for developing antitumor agents. Herein, we synthesized and evaluated a series of novel chiral dipeptide thioureas containing an α-aminophosphonate moiety as antitumor agents. Finally, we developed novel dipeptide thioureas11dand11fthat showed comparable inhibition with that of Cisplatin against BGC-823 and A-549 cells, respectively.
authors.affiliation: Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang 550004, Guizhou, China. liujingz@126.com.|Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang 550004, Guizhou, China. liujingz@126.com.|School of Pharmacy, Guizhou Medical University, Guiyang 550004, Guizhou, China. liujingz@126.com.|National Engineering Research Center of Miao's Medicines, Guizhou Medical University, Guiyang 550004, Guizhou, China. liujingz@126.com.|School of Pharmacy, Zunyi Medical College, Zunyi 563000, Guizhou, China. liujingz@126.com.
authors.forename: Jingzi
authors.initials: J
authors.lastname: Liu
authors.affiliation: Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang 550004, Guizhou, China. m17785598945@163.com.|Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang 550004, Guizhou, China. m17785598945@163.com.|School of Pharmacy, Guizhou Medical University, Guiyang 550004, Guizhou, China. m17785598945@163.com.|National Engineering Research Center of Miao's Medicines, Guizhou Medical University, Guiyang 550004, Guizhou, China. m17785598945@163.com.
authors.forename: Peng
authors.initials: P
authors.lastname: Liao
authors.affiliation: School of Pharmacy, Zunyi Medical College, Zunyi 563000, Guizhou, China. hjfgmu@21cn.com.
authors.forename: Junfeng
authors.initials: J
authors.lastname: Hu
authors.affiliation: Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang 550004, Guizhou, China. Zhhgmu@21cn.com.|Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang 550004, Guizhou, China. Zhhgmu@21cn.com.|School of Pharmacy, Guizhou Medical University, Guiyang 550004, Guizhou, China. Zhhgmu@21cn.com.|National Engineering Research Center of Miao's Medicines, Guizhou Medical University, Guiyang 550004, Guizhou, China. Zhhgmu@21cn.com.
authors.forename: Hong
authors.initials: H
authors.lastname: Zhu
authors.affiliation: Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang 550004, Guizhou, China. yonglinwang@gmc.edu.cn.|Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang 550004, Guizhou, China. yonglinwang@gmc.edu.cn.|School of Pharmacy, Guizhou Medical University, Guiyang 550004, Guizhou, China. yonglinwang@gmc.edu.cn.|National Engineering Research Center of Miao's Medicines, Guizhou Medical University, Guiyang 550004, Guizhou, China. yonglinwang@gmc.edu.cn.
authors.forename: Yonglin
authors.initials: Y
authors.lastname: Wang
authors.affiliation: Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang 550004, Guizhou, China. m13765113985@163.com.|Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang 550004, Guizhou, China. m13765113985@163.com.|School of Pharmacy, Guizhou Medical University, Guiyang 550004, Guizhou, China. m13765113985@163.com.|National Engineering Research Center of Miao's Medicines, Guizhou Medical University, Guiyang 550004, Guizhou, China. m13765113985@163.com.
authors.forename: Yongjun
authors.initials: Y
authors.lastname: Li
authors.affiliation: School of Basic Medicine, Guizhou Medical University, Guiyang 550004, Guizhou, China. yanli@gmc.edu.cn.
authors.forename: Yan
authors.initials: Y
authors.lastname: Li
authors.affiliation: Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang 550004, Guizhou, China. binhe@gmc.edu.cn.|Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang 550004, Guizhou, China. binhe@gmc.edu.cn.|School of Pharmacy, Guizhou Medical University, Guiyang 550004, Guizhou, China. binhe@gmc.edu.cn.|National Engineering Research Center of Miao's Medicines, Guizhou Medical University, Guiyang 550004, Guizhou, China. binhe@gmc.edu.cn.
authors.forename: Bin
authors.initials: B
authors.lastname: He
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004151:Dipeptides / Q000737:chemistry*; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D063065:Organophosphonates / Q000737:chemistry*; D013890:Thiourea / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D004151:Dipeptides; D063065:Organophosphonates; D013890:Thiourea
keywords: aminophosphonate; antitumor agents; dipeptide; synthesis; thiourea