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Bulletin of the Korean Chemical Society
Article

Study on Anti‐Proliferative Activity in Cancer Cells and Preliminary Structure–Activity Relationship of Pseudo‐Peptide Chiral Thioureas

Peng Liao

School of Pharmacy, Guizhou Medical University; Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, Ministry of Education; Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, 550004 Guizhou, China

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Shi‐Qin Hu

School of Pharmacy, Guizhou Medical University; Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, Ministry of Education; Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, 550004 Guizhou, China

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Hong Zhang

The Affiliated Hospital of Guizhou Medical University, Guiyang, 550004 Guizhou, China

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Liang‐Bi Xu

The Affiliated Hospital of Guizhou Medical University, Guiyang, 550004 Guizhou, China

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Jing‐Zi Liu

Corresponding Author

E-mail address: liujingz@126.com

E-mail address: 435096064@qq.com

School of Pharmacy, Guizhou Medical University; Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, Ministry of Education; Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, 550004 Guizhou, China

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Bin He

School of Pharmacy, Guizhou Medical University; Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, Ministry of Education; Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, 550004 Guizhou, China

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Shang‐Gao Liao

School of Pharmacy, Guizhou Medical University; Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, Ministry of Education; Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, 550004 Guizhou, China

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Yong‐Jun Li

School of Pharmacy, Guizhou Medical University; Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, Ministry of Education; Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, 550004 Guizhou, China

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First published: 09 February 2018
Cited by: 2
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Abstract

In our previous studies, we have shown that thiourea compounds containing phosphate esters have potent antitumor activity and can be used as a novel strategy for the development of antitumor agents. Herein, a series of novel phosphonate thioureas 5–38 have been synthesized, which were fully characterized by 1H NMR, 13C NMR spectrum, elemental analysis. Three human cancer cell lines (Bcap‐37, BGC‐823, and PC‐3) have been used to investigate these compounds’ antitumor activities. After the summarization of the structure–activity relationships, we found that the variation of R, R1, and R2 in these novel phosphonate thioureas contribute to the antitumor activities. All these SAR‐guided efforts may lead to novel antitumor drugs in the market in the near future.

Number of times cited according to CrossRef: 2

  • , Design, Synthesis, and Cytotoxic Activity of 3‐Aryl‐N‐hydroxy‐2‐(sulfonamido)propanamides in HepG2, HT‐1080, KB, and MCF‐7 Cells, Chemistry & Biodiversity, 16, 4, (2019).
  • , Co-ligand induced chiral recognition of N-thiophosphorylated thioureas in crystalline Ni(II) complexes, Crystal Growth & Design, 10.1021/acs.cgd.9b00446, (2019).