Title
Chemistry of Ecteinascidins. Part 5: An Additional Proof of Cytotoxicity Evaluation of Ecteinascidin 770 Derivatives
Author
Ryoko Toyoshima, Nanae Mori, Toshihiro Suzuki, Witaya Lowtangkitcharoen, Khanit Suwanborirux, Naoki Saito
Year
2016
Journal
Chemical and Pharmaceutical Bulletin
Abstract
Eleven 2′-N-acyl derivatives (5a–k) were prepared from ecteinascidin 770 (Et 770: 1b) viaknown 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.
Instrument
J-820
Keywords
Circular dichroism, Stereochemistry, Pharmaceutical