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

…, T Hinosawa, Y Nakagawa, T Hasuda, K Takeya

Index: Hitotsuyanagi, Yukio; Miyazawa, Akihiro; Hinosawa, Taka-Aki; Nakagawa, Yoshie; Hasuda, Tomoyo; Takeya, Koichi Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 24 p. 6728 - 6731

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Abstract

Abstract An aza-cycloisodityrosine analogue of RA-VII, 3, was designed and synthesized. The key aza-cycloisodityrosine unit was prepared by copper (II)-acetate-mediated intramolecular phenylamine/arylboronic acid coupling of dipeptide followed by connection with the tetrapeptide segment to afford a hexapeptide. Subsequent macrocyclization of the hexapeptide with EDC· HCl and HOOBt under dilute conditions gave 3. Analogue 3 ...