Synthesis and biological activity of flavanone derivatives
Synthesis and biological activity of flavanone derivatives
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DOI：
10.1016/j.bmcl.2010.07.090
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发表时间：
2010-09-15
影响因子：
2.7
通讯作者：
Li, Qing Shan
中科院分区：
文献类型：
--
作者：
Shi, Lei;Feng, Xiu E.;Li, Qing Shan
用简便的方法合成了一系列新的杜鹃素黄烷酮衍生物。体外抗人Bel-7402、HL-60、BGC-823和KB细胞活性和蛋白酪氨酸激酶（PTK）抑制活性。使用过氧化氢（H2 O2）诱导的人脐静脉内皮细胞损伤检测其细胞保护活性。以粉防己碱为阳性对照药，采用MTT法检测其体外抗动脉粥样硬化活性。所有化合物的结构均经H-1、C-13 NMR和ESI-MS确证，大部分化合物具有良好的药理活性，并对其初步构效关系进行了描述。(c)2010爱思唯尔有限公司版权所有。
A series of new flavanone derivatives of farrerol was synthesized by a convenient method. The in vitro anti-tumor activity of these compounds was evaluated against human Bel-7402, HL-60, BGC-823 and KB cell lines, the protein tyrosine kinase (PTK) inhibitor activity was also tested. Their cytoprotective activity was tested using hydrogen peroxide (H2O2)-induced injury in human umbilical vein endothelial cells. Their in vitro anti-atherosclerosis activity was tested on vascular smooth muscle cells by the MTT method using tetrandrine as a positive contrast drug. The structures of all compounds synthesized were confirmed by H-1, C-13 NMR and ESI-MS. Most of the compounds exhibited good pharmacological activity and the preliminary structure-activity relationships were described. (c) 2010 Elsevier Ltd. All rights reserved.