Abstract: 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.
This is an open access article distributed under the
Creative Commons Attribution License which permits unrestricted use, distribution,
and reproduction in any medium, provided the original work is properly cited.
Export to BibTeX
MDPI and ACS Style
Sun, T.; Li, Z.-L.; Tian, H.; Wang, S.-C.; Cai, J. Synthesis and Biological Evaluation of Novel 1-Alkyltryptophan Analogs as Potential Antitumor Agents. Molecules 2009, 14, 5339-5348.
Sun T, Li Z-L, Tian H, Wang S-C, Cai J. Synthesis and Biological Evaluation of Novel 1-Alkyltryptophan Analogs as Potential Antitumor Agents. Molecules. 2009; 14(12):5339-5348.
Sun, Ting; Li, Zhao-Long; Tian, Hua; Wang, Shih-Chen; Cai, Jiong. 2009. "Synthesis and Biological Evaluation of Novel 1-Alkyltryptophan Analogs as Potential Antitumor Agents." Molecules 14, no. 12: 5339-5348.