Literature

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.

DOI： 10.1016/j.bmcl.2008.10.064

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

Bioorganic & Medicinal Chemistry Letters 2008.0

Synthesis of [Tyr-5-Ψ(CH2NMe)-Tyr-6]RA-VII, a reduced peptide bond analogue of RA-VII, an antitumor bicyclic hexapeptide

Bioorganic & Medicinal Chemistry Letters 2012.0

Aza-cycloisodityrosine analogue of RA-VII, an antitumor bicyclic hexapeptide

Bioorganic & Medicinal Chemistry Letters 2013.0

Per-N-methylated analogues of an antitumor bicyclic hexapeptide RA-VII

Bioorganic & Medicinal Chemistry 2011.0

Preparation and antitumor activity of [N-alkyl-Ala2]RA-VII, antitumor cyclic hexapeptide

Bioorganic & Medicinal Chemistry Letters 1994.0

Isolation, structural elucidation, and synthesis of RA-XVII, a novel bicyclic hexapeptide from Rubia cordifolia, and the effect of side chain at residue 1 upon the conformation and cytotoxic activity