Chemistry of Ecteinascidins. Part 5: An Additional Proof of Cytotoxicity Evaluation of Ecteinascidin 770 Derivatives

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  • Toyoshima Ryoko
    Graduate School of Pharmaceutical Sciences, Meiji Pharmaceutical University
  • Mori Nanae
    Graduate School of Pharmaceutical Sciences, Meiji Pharmaceutical University
  • Suzuki Toshihiro
    Graduate School of Pharmaceutical Sciences, Meiji Pharmaceutical University
  • Lowtangkitcharoen Witaya
    Center for Bioactive Natural Products from Marine Organisms and Endophytic Fungi (BNPME), Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Chulalongkorn University
  • Suwanborirux Khanit
    Center for Bioactive Natural Products from Marine Organisms and Endophytic Fungi (BNPME), Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Chulalongkorn University
  • Saito Naoki
    Graduate School of Pharmaceutical Sciences, Meiji Pharmaceutical University

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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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