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  • Title: Chemistry of Ecteinascidins. Part 5: An Additional Proof of Cytotoxicity Evaluation of Ecteinascidin 770 Derivatives.
    Author: Toyoshima R, Mori N, Suzuki T, Lowtangkitcharoen W, Suwanborirux K, Saito N.
    Journal: Chem Pharm Bull (Tokyo); 2016; 64(7):966-9. PubMed ID: 27373655.
    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.
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