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

Bulletin of the Korean Chemical Society

ShiQin Hu¹  Hong Zhang²  Peng Liao³  LiangBi Xu⁴ 

[1] 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;School of Pharmacy, Guizhou Medical University;The Affiliated Hospital of Guizhou Medical University Guiyang 550004 Guizhou, China

关键词: Thiourea;    Phosphonate;    Pseudo‐;    peptide;    Antitumor agents;    Structure–;    function relationship;    Human cancer cell lines;   

DOI  :  10.1002/bkcs.11383

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

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.

【 授权许可】

Unknown