title: Asymmetric synthesis and cytotoxicity of (-)-saframycin A analogues.
abstract: (-)-Saframycin A and its nineteen analogues were prepared from L-tyrosine in 24 steps, and their structures were confirmed through NMR and HRMS. The cytotoxicities of these compounds were tested against HCT-8, BEL-7402, Ketr3, A2780, MCF-7, A549, BGC-803, Hela, HELF and KB cell lines. The IC(50) values of the cytotoxicity of most compounds were at the level of nM. Compound 7d with 2-furan amide side chain showed the most potent cytotoxicity of all these compounds with an average IC(50) value of 6.06 nM.
authors.affiliation: State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing, PR China.
authors.forename: Wenfang
authors.initials: W
authors.lastname: Dong
authors.forename: Wei
authors.initials: W
authors.lastname: Liu
authors.forename: Zheng
authors.initials: Z
authors.lastname: Yan
authors.forename: Xiangwei
authors.initials: X
authors.lastname: Liao
authors.forename: Baohe
authors.initials: B
authors.lastname: Guan
authors.forename: Nan
authors.initials: N
authors.lastname: Wang
authors.forename: Zhanzhu
authors.initials: Z
authors.lastname: Liu
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007546:Isoquinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D009369:Neoplasms / Q000188:drug therapy; D013302:Streptomyces / Q000737:chemistry
chemical_list: D000903:Antibiotics, Antineoplastic; D007546:Isoquinolines; C026925:saframycin A