Study on Anti‐Proliferative Activity in Cancer Cells and Preliminary Structure–Activity Relationship of Pseudo‐Peptide Chiral Thioureas
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
- Duanyang Shao, Guo‐Ning Zhang, Weixiao Niu, Ziqiang Li, Mei Zhu, Juxian Wang, Donghui Li and Yucheng Wang, 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).
- Olga N. Kataeva, Kirill E. Metlushka, Zilya R. Yamaleeva, Kamil A. Ivshin, Airat G. Kiiamov, Olga A. Lodochnikova, Kristina A. Nikitina, Dilyara N. Sadkova, Lyudmila N. Punegova, Alexandra D. Voloshina, Anna P. Lyubina, Anastasiya S. Sapunova, Oleg G. Sinyashin and Vladimir A. Alfonsov, Co-ligand induced chiral recognition of N-thiophosphorylated thioureas in crystalline Ni(II) complexes, Crystal Growth & Design, 10.1021/acs.cgd.9b00446, (2019).