Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593309 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
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 showed significant cytotoxic activity against human promyelocytic leukemia HL-60 cells and human colon carcinoma HCT-116 cells, but its activity was weaker than that of parent peptide RA-VII (1).
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yukio Hitotsuyanagi, Akihiro Miyazawa, Taka-aki Hinosawa, Yoshie Nakagawa, Tomoyo Hasuda, Koichi Takeya,