【摘 要】
：
Glutathione S-transferases π (GSTπ) catalyzes the conjugation of glutathione (GSH) to an electrophilic center of endogenous and exogenous compounds and is frequently over-expressed in many human tumor
【机 构】
：
Center of Drug Discovery,China Pharmaceutical University,Nanjing 210009
【出 处】
：
第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
论文部分内容阅读
Glutathione S-transferases π (GSTπ) catalyzes the conjugation of glutathione (GSH) to an electrophilic center of endogenous and exogenous compounds and is frequently over-expressed in many human tumors.1 O2-arylated diazeniumdiolates represent a promising class of nitric oxide (NO) donors,which,after proper modification and upon activation by GSH/GSTπ,selectively release high level of NO in cancer cells.2 Herein,we report the synthesis of oleanolic acid (OA)derivatives by connecting O2-arylated diazeniumdiolates to the 3-OH of OA,and evaluation of their anti-HCC activity.In vitro assessment indicated that compound Npq possessed potent and selective cytotoxicity against HCC cells with IC50 between 1.4and 2.3 μM.Importantly,the high levels of NO produced in HCC cells played an essential role in Npqs activity,which was significantly abrogated by NO quencher haemoglobin.
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