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Molecules 2017, 22(2), 238; doi:10.3390/molecules22020238

Synthesis and Antitumor Activities of Chiral Dipeptide Thioureas Containing an Alpha-Aminophosphonate Moiety

1,2,3,4,5,* , 1,2,3,4
,
5
,
1,2,3,4
,
1,2,3,4
,
1,2,3,4
,
6,* and 1,2,3,4,*
1
Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang 550004, Guizhou, China
2
Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang 550004, Guizhou, China
3
School of Pharmacy, Guizhou Medical University, Guiyang 550004, Guizhou, China
4
National Engineering Research Center of Miao’s Medicines, Guizhou Medical University, Guiyang 550004, Guizhou, China
5
School of Pharmacy, Zunyi Medical College, Zunyi 563000, Guizhou, China
6
School of Basic Medicine, Guizhou Medical University, Guiyang 550004, Guizhou, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 18 December 2016 / Revised: 26 January 2017 / Accepted: 30 January 2017 / Published: 16 February 2017
View Full-Text   |   Download PDF [507 KB, uploaded 16 February 2017]   |  

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 thioureas 11d and 11f that showed comparable inhibition with that of Cisplatin against BGC-823 and A-549 cells, respectively. View Full-Text
Keywords: dipeptide; thiourea; aminophosphonate; synthesis; antitumor agents dipeptide; thiourea; aminophosphonate; synthesis; antitumor agents
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Liu, J.; Liao, P.; Hu, J.; Zhu, H.; Wang, Y.; Li, Y.; Li, Y.; He, B. Synthesis and Antitumor Activities of Chiral Dipeptide Thioureas Containing an Alpha-Aminophosphonate Moiety. Molecules 2017, 22, 238.

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