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3- (hydroxy substituted benzoyl) and 3- (hydroxy substituted cinnamoyl) synthesis and antitumor activity of oleanolic acid derivatives

Author: WuXiaoDong
Tutor: XuYongNan
School: Shenyang Pharmaceutical University
Course: Medicinal Chemistry
Keywords: oleanolic acid derivates antitumor
CLC: R91
Type: Master's thesis
Year: 2007
Downloads: 24
Quote: 0
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Abstract


As pentacyclic triterpenoids, oleanolic acid are ubiquitous in the plant kingdom and exhibit various biological activities,Nineteen derivatives of oleanolic acid were designed and synthesized, nine of which are intermediate, other ten are target compound. All there compound were characterized by means of IR. 1H NMR, 13C NMR and MS.The cytotoxic activities of these compound against tumor cell (A549) were evaluated and cisplatine (DPP) was the positive control. It came to the conclusion that BO 15 (IC50=3.78μg/mL) and BO 19 (IC50=4.09μg/mL) showed potent inhibition effect on the growth of the tumor cell. On the basis of A549 inhibitory activity of the target compounds, structure-activity relationships discussion was taken, which will give us some useful information in the design of new drugs. Further synthesize and pharmacological test are underway.

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