Tetrahedron

Synthesis and biological activities of [N-MeLeu 5]-and [N-MePhe 5]-didemnin B

…, MD Vera, X Ding, D Xiao, C Wei-Chuan, MM Joullié

Index: Pfizenmayer, Amy J.; Ramanjulu, Joshi M.; Vera, Matthew D.; Ding, Xiaobin; Xiao, Dong; Chen, Wei-Chuan; Joullie, Madeleine M. Tetrahedron, 1999 , vol. 55, # 2 p. 313 - 334

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Citation Number: 25

Abstract

Based on information from X-ray, NMR, and SAR data, the N, O-diMeTyr5 unit of didemnin B was believed to be important for biological activity. To determine the importance of aromaticity and the role of the methoxy group in this unit, two analogs were synthesized in which the N, O-diMeTyr5 moiety was replaced with N-MeLeu and N-MePhe. Preliminary testing showed that the analogs retained antitumor activity and the ability to inhibit protein ...