Synthesis and Anti-angiogenesis Activities of Ursolic Acid Derivatives

Abstract

Abstract: Twenty-four derivatives of ursolic acid modified at C3 and C28 were designed and synthesized for the investigation of the structure-activity relationship of ursolic acid(1) against angiogenesis. All the compounds were characterized by 1H NMR, 13C NMR, MS and HR-MS. HUVEC was used as an angiogenesis target cell and A549, Bel-7402 and MCF-7 were as cancer target cells and the antiproliferative activity was assayed by MTT method. The results show that compounds 5, 9, 12e and 14e possess the selectively antiproliferative activity of HUVEC, meanwhile, compounds 12a and 13h are more active than compound 1 against the proliferation of HUVEC. Therefore, it is possible that more potent and selective angiogenesis inhibitors of ursolic acid derivatives could be discovered by suitable modification at C28 position of ursolic acid. These data suggest that ursolic acid and its derivatives represent a promising lead structural core to discover a new class of antiangiogenesis agents.

Key words: Ursolic acid, Derivative, Anti-angigenesis, Antiproliferation

TrendMD:

ZHANG Wen-Juan, CHEN Shao-Peng, LU Xin, ZHOU Guo-Chun* . Synthesis and Anti-angiogenesis Activities of Ursolic Acid Derivatives[J]. Chem. J. Chinese Universities, 2010, 31(11): 2206.

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