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

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 o...

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Detalles Bibliográficos
Autores principales: Liu, Jingzi, Liao, Peng, Hu, Junfeng, Zhu, Hong, Wang, Yonglin, Li, Yongjun, Li, Yan, He, Bin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155911/
https://www.ncbi.nlm.nih.gov/pubmed/28212338
http://dx.doi.org/10.3390/molecules22020238
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author Liu, Jingzi
Liao, Peng
Hu, Junfeng
Zhu, Hong
Wang, Yonglin
Li, Yongjun
Li, Yan
He, Bin
author_facet Liu, Jingzi
Liao, Peng
Hu, Junfeng
Zhu, Hong
Wang, Yonglin
Li, Yongjun
Li, Yan
He, Bin
author_sort Liu, Jingzi
collection PubMed
description 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.
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spelling pubmed-61559112018-11-13 Synthesis and Antitumor Activities of Chiral Dipeptide Thioureas Containing an Alpha-Aminophosphonate Moiety Liu, Jingzi Liao, Peng Hu, Junfeng Zhu, Hong Wang, Yonglin Li, Yongjun Li, Yan He, Bin Molecules Article 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. MDPI 2017-02-16 /pmc/articles/PMC6155911/ /pubmed/28212338 http://dx.doi.org/10.3390/molecules22020238 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Liu, Jingzi
Liao, Peng
Hu, Junfeng
Zhu, Hong
Wang, Yonglin
Li, Yongjun
Li, Yan
He, Bin
Synthesis and Antitumor Activities of Chiral Dipeptide Thioureas Containing an Alpha-Aminophosphonate Moiety
title Synthesis and Antitumor Activities of Chiral Dipeptide Thioureas Containing an Alpha-Aminophosphonate Moiety
title_full Synthesis and Antitumor Activities of Chiral Dipeptide Thioureas Containing an Alpha-Aminophosphonate Moiety
title_fullStr Synthesis and Antitumor Activities of Chiral Dipeptide Thioureas Containing an Alpha-Aminophosphonate Moiety
title_full_unstemmed Synthesis and Antitumor Activities of Chiral Dipeptide Thioureas Containing an Alpha-Aminophosphonate Moiety
title_short Synthesis and Antitumor Activities of Chiral Dipeptide Thioureas Containing an Alpha-Aminophosphonate Moiety
title_sort synthesis and antitumor activities of chiral dipeptide thioureas containing an alpha-aminophosphonate moiety
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155911/
https://www.ncbi.nlm.nih.gov/pubmed/28212338
http://dx.doi.org/10.3390/molecules22020238
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