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

Ryoko Toyoshima; Nanae Mori; Toshihiro Suzuki; Witaya Lowtangkitcharoen; Khanit Suwanborirux; Naoki Saito

doi:10.1248/cpb.c16-00192

Special Collection of Papers: Notes

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

Ryoko Toyoshima, Nanae Mori, Toshihiro Suzuki, Witaya Lowtangkitcharoen, Khanit Suwanborirux, Naoki Saito

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Keywords: marine natural product, transformation, ecteinascidin, cytotoxicity, structure–activity relationship study

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2016 Volume 64 Issue 7 Pages 966-969

DOI https://doi.org/10.1248/cpb.c16-00192

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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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