960化工网
Total synthesis and evaluation of Wnt signal inhibition of melleumin A and B, and their derivatives†
Midori A. Arai,Shuwa Hanazawa,Yujiro Uchino,Xiaofan Li,Masami Ishibashi
Organic & Biomolecular Chemistry Pub Date : 09/23/2010 00:00:00 , DOI:10.1039/C0OB00352B
Abstract

The total synthesis of melleumin A (1), a novel cyclic depsipeptide isolated from the myxomycete Physarum melleum, and 3-epi-melleumin A (6) was achieved. Melleumin A-like compounds were also designed and synthesized; analysis of these melleumin A-like compounds showed moderate Wnt signal inhibition. Comparison of the inhibition activity of melleumin B and its three epimers, melleumin A, 3-epi-melleumin A and three melleumin A-like compounds led to further investigation of the structural conformation of the active molecules. The scaffold of melleumin is a potential target in the search for “peptide-like” Wnt signaling inhibitors.

Graphical abstract: Total synthesis and evaluation of Wnt signal inhibition of melleumin A and B, and their derivatives
平台客服
平台客服
平台在线客服