title: Chemistry of Ecteinascidins. Part 5: An Additional Proof of Cytotoxicity Evaluation of Ecteinascidin 770 Derivatives.
abstract: Eleven 2'-N-acyl derivatives (5a-k) were prepared from ecteinascidin 770 (Et 770: 1b) via known 18,6'-O-bisallyl-protected compound (3) in three steps. Their in vitro cytotoxicities were determined by measuring IC50 values against human cell lines HCT116 and DU145. 5-Isoxazolecarboylamide derivative (5i) and 4-methoxybenzoylamide derivative (5k) were found to be promising leads for further optimization.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Meiji Pharmaceutical University.
authors.forename: Ryoko
authors.initials: R
authors.lastname: Toyoshima
authors.forename: Nanae
authors.initials: N
authors.lastname: Mori
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Suzuki
authors.forename: Witaya
authors.initials: W
authors.lastname: Lowtangkitcharoen
authors.forename: Khanit
authors.initials: K
authors.lastname: Suwanborirux
authors.forename: Naoki
authors.initials: N
authors.lastname: Saito
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D006576:Heterocyclic Compounds, 4 or More Rings / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D007546:Isoquinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D006576:Heterocyclic Compounds, 4 or More Rings; D007546:Isoquinolines; C464992:ecteinascidin 770