Synthesis and Biological Evaluation of Novel 1-Alkyltryptophan Analogs as Potential Antitumor Agents

Molecules

Ting Sun¹  Zhao-Long Li¹  Hua Tian¹  Shih-Chen Wang¹ 

[1] ¹Department of Nuclear Medicine, Peking Union Medical College & Chinese Academy of Medical Sciences, Peking Union Medical College Hospital, Beijing 100730, China ²Department of Chemistry, Tsinghua University, Beijing 100084, China ³Department of Pathology, Shanghai Jiao Tong University School of Medicine, Shanghai 200025, China

关键词: tryptophan analogs;    cytotoxicity;    MTT;   

DOI  :  10.3390/molecules14125339

来源: mdpi

【 摘 要 】

To seek novel antitumor agents, we designed and synthesized new 1-tryptophan analogs based on tryptophan catabolism. 1-Alkyltryptophan analogues including 1-ethyltryptophan (1-ET), 1-propyltryptophan (1-PT), 1-isopropyltryptophan (1-isoPT) and 1-butyltryptophan (1-BT) were synthesized from tryptophan. We examined whether those compounds had the antiproliferative effects on SGC7901 and HeLa cells line by using MTT assay in vitro, respectively. Compared to tryptophan, all targeted compounds efficiently inhibited proliferation of two cancer cell lines at 2 mmol/L for 48 hours. Among these tryptophan analogs, 1-BT showed the most powerful cytotoxicity against SGC7901 and HeLa cells at 1 mmol/L and 2 mmol/L concentration. These data suggest that some specific tryptophan analogs could be developed as potential anti-neoplastic agents.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.