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Title of Article Chemistry of Ecteinascidins. Part 4. Preparation of 2'-N-Acyl Ecteinascidin770 Derivatives with Improved Cytotoxicity Profiles 
Date of Acceptance 1 October 2013 
     Title of Journal Chem. Pharm .Bull 
     Institute of Journal The Pharmaceutical Society of Japan 
     Volume 2013 
     Issue 61 
     Month 10
     Year of Publication 2013 
     Page 1052-1064 
     Abstract We report herein eleven 2-N-acyl derivatives that were prepared from ecteinascidin 770 (Et 770: 1b) via 18,6-O-bisallyl protected compound (4) in excellent yields. 2-N-Acyl derivatives (6a–k) generally showed higher cytotoxicity than 1b. Among them, 3-quinolineacyl derivative (6g) and 4-fluorocinnamoyl derivative (6h) exhibited approximately 50- and 70-fold higher cytotoxicity to the HCT116 human colon carcinoma cell line, respectively, than 1b. Both compounds are potent inhibitors of the in vitro growth of several tumor cells and are therefore promising leads for further optimization. We also report the transformation of 1b into Et 788 (3), which is the first example of an ecteinascidin derivative having a primary amide at C-21 position. 
     Keyword ecteinascidin; marine natural product; structure–activity relationship study; transformation; cytotoxicity 
535150053-5 Miss WAREE PANGKRUANG [Main Author]
Pharmaceutical Sciences Master's Degree

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