title: Synthesis and biological evaluation of novel 1-alkyl-tryptophan analogs as potential antitumor agents.
abstract: To seek novel antitumor agents, we designed and synthesized new 1-tryptophan analogs based on tryptophan catabolism. 1-Alkyl-tryptophan 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.
authors.affiliation: Department of Nuclear Medicine, Peking Union Medical College & Chinese Academy of Medical Sciences, Peking Union Medical College Hospital, Beijing 100730, China. beibeisun2008@163.com
authors.forename: Ting
authors.initials: T
authors.lastname: Sun
authors.forename: Zhao-Long
authors.initials: ZL
authors.lastname: Li
authors.forename: Hua
authors.initials: H
authors.lastname: Tian
authors.forename: Shih-Chen
authors.initials: SC
authors.lastname: Wang
authors.forename: Jiong
authors.initials: J
authors.lastname: Cai
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D004797:Enzyme-Linked Immunosorbent Assay; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D014364:Tryptophan / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D014364:Tryptophan