Structure--activity relationships of side-chain modified didemnins.

Abstract

The synthesis and antitumor activity of a novel didemnin B analogue containing a psi[CH2NH] amide bond surrogate between N-Me-D-Leu7 and Pro8 are reported. The analogue shows activity (GI50 = 4 nM) comparable to that of didemnin B (GI50 = 13 nM) in the NCI-60 tumor cell screen. This result, along with new data from previously reported synthetic didemnin analogues, is discussed within the context of the side-chain SAR for didemnins.

• Authors: X Ding, M D Vera, B Liang, Y Zhao, M S Leonard, M M Joullié
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 11 Issue 2 Pg. 231-4 (Jan 22 2001) ISSN: 0960-894X [Print] England
• PMID: 11206466 (Publication Type: Journal Article, Research Support, U.S. Gov't, Non-P.H.S., Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Antineoplastic Agents
• Depsipeptides
• Peptides, Cyclic
• didemnins

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Combinatorial Chemistry Techniques
• Depsipeptides
• Drug Screening Assays, Antitumor
• Humans
• Molecular Mimicry
• Peptides, Cyclic (chemical synthesis, chemistry, pharmacology)
• Structure-Activity Relationship
• Tumor Cells, Cultured (drug effects)