Hitotsuyanagi Yukio, Motegi Shuichi, Hasuda Tomoyo, Takeya Koichi
School of Pharmacy, Tokyo University of Pharmacy and Life Science, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
Org Lett. 2004 Apr 1;6(7):1111-4. doi: 10.1021/ol040005r.
We prepared an analogue of an antitumor bicyclic hexapeptide RA-VII whose amide configuration between residues 2 and 3 was fixed to cis by incorporating a triazole cis-amide bond surrogate. This analogue was shown, by NMR studies, to take almost the same conformation as that of the minor conformer of RA-VII. It showed no cytotoxic activity.
我们制备了一种抗肿瘤双环六肽RA-VII的类似物，通过引入三唑顺式酰胺键替代物，将2位和3位残基之间的酰胺构型固定为顺式。通过核磁共振研究表明，该类似物的构象与RA-VII的次要构象几乎相同。它没有显示出细胞毒性活性。
