2. Academic Validation
  3. Design and synthesis of a bis(cycloisodityrosine) analogue of RA-VII, an antitumor bicyclic hexapeptide

Design and synthesis of a bis(cycloisodityrosine) analogue of RA-VII, an antitumor bicyclic hexapeptide

  • Bioorg Med Chem Lett. 2008 Dec 15;18(24):6458-61. doi: 10.1016/j.bmcl.2008.10.064.
Ji-Ean Lee 1,  Yukio Hitotsuyanagi,  Yoshie Nakagawa,  Saori Kato,  Haruhiko Fukaya,  Koichi Takeya
Affiliations

Affiliation

  • 1 School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
PMID: 18993061 DOI: 10.1016/j.bmcl.2008.10.064
Abstract

An analogue of an antitumor bicyclic hexapeptide RA-VII was prepared, in which the Ala-2 and Tyr-3 residues of RA-VII were replaced by a cycloisodityrosine unit. In the crystalline state, the peptide backbone structures and the side-chain conformations at Tyr-3, Tyr-5, and Tyr-6 of this analogue and of RA-II were very similar. This analogue, however, showed much weaker cytotoxicity against P-388 leukemia cells than parent RA-VII.

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