Targeting cancer cells with oleanolic and ursolic acid derived hydroxamates

详细信息    查看全文

• 作者：Jana Wiemann ; Lucie Heller ; René ; Csuk ; ^{rene.csuk@chemie.uni-halle.de" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Triterpenes ; Oleanolic acid ; Ursolic acid ; Hydroxamates ; SRB assay ; Cancer
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 February 2016
• 年：2016
• 卷：26
• 期：3
• 页码：907-909
• 全文大小：280 K

文摘

Oleanolic and ursolic acid derived hydroxamates were easily obtained from their parent compounds; they were screened for their cytotoxicity applying SRB assays employing several human tumor cell lines. Low EC₅₀ values were determined for compounds in which the nitrogen as well as the oxygen in the hydroxamic acid part still holds acidic hydrogens. Thus, ursolic acid derived compounds having at least an OH and/or NH moiety in the hydroxamate part of the molecule showed good cytotoxicity but they are significantly less selective for the tumor cells than oleanolic acid derived compounds. Good results were determined for oleanolic acid derived 7 for tumor cell lines 518A2 (melanoma, EC₅₀ = 3.3 μM), A2780 (ovarian carcinoma, EC₅₀ = 3.4 μM) and HT29 (colon adenocarcinoma, EC₅₀ = 5.6 μM) while being significantly less cytotoxic for fibroblasts (EC₅₀ = 20.4 μM).