Document Report Card

ID: ALA1140707

Journal: J Med Chem

Title: Structural modification of an angiogenesis inhibitor discovered from traditional Chinese medicine and a structure-activity relationship study.

Authors: Yang SP, Cai YJ, Zhang BL, Tong LJ, Xie H, Wu Y, Lin LP, Ding J, Yue JM.

Abstract: Pseudolaric acid B (PAB), discovered as a promising angiogensis inhibitor, was served as the anticancer drug lead, and a series of its derivatives were synthesized. Among them, some derivatives, such as 13c- 13k, exhibited potent inhibition on the HMEC-1 cell proliferation and strong cytotoxic activities against the tested six tumor cell lines. The PAB derivatives 13c- 13k also showed significant and specific inhibition on HMEC-1 cell migration in vitro, and only 13d expressed moderate activity against HMEC-1 cell tube formation. The in vitro anticancer tests of the selected natural PAB analogs and the structurally modified PAB derivatives have led to the establishment of a clear structure-activity relationship.

CiteXplore: 18078313

DOI: 10.1021/jm070906g