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

1
Department of Nuclear Medicine, Peking Union Medical College & Chinese Academy of Medical Sciences, Peking Union Medical College Hospital, Beijing 100730, China
2
Department of Chemistry, Tsinghua University, Beijing 100084, China
3
Department of Pathology, Shanghai Jiao Tong University School of Medicine, Shanghai 200025, China
*
Author to whom correspondence should be addressed.
Molecules 2009, 14(12), 5339-5348; https://doi.org/10.3390/molecules14125339
Received: 28 November 2009 / Revised: 16 December 2009 / Accepted: 17 December 2009 / Published: 18 December 2009
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. View Full-Text
Keywords: tryptophan analogs; cytotoxicity; MTT tryptophan analogs; cytotoxicity; MTT
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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.

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