Synthesis and biological activities of [N-MeLeu5] didemnin B

✍ Scribed by Amy J. Pfizenmayer; Joshi Ramanjulu; Matthew D. Vera; Xiaobin Ding; Dong Xiao; Wei-Chuan Chen; Madeleine M. Joullié

• Book ID: 104364652
• Publisher: Elsevier Science
• Year: 1996
• Tongue: English
• Weight: 215 KB
• Volume: 6
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/s0960-894x(96)00506-9

✦ Synopsis

Based on information from X-ray, NMR, and SAR data, the N,O-diMeTyr 5 unit of didemnin B was believed to interact with receptors. To ascertain the importance of this unit, an analog was synthesized in which the N,O-diMeTyr 5 moiety was replaced with N-MeLeu. Preliminary biological testing showed that the analog retained antitumor activity and the ability to inhibit protein biosynthesis.