Synthesis and antiproliferative activity of novel selenoester derivatives
Synthesis and antiproliferative activity of novel selenoester derivatives
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DOI：
10.1016/j.ejmech.2013.11.034
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发表时间：
2014-02-12
影响因子：
6.7
通讯作者：
Sanmartin, Carmen
中科院分区：
文献类型：
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作者：
Dominguez-Alvarez, Enrique;Plano, Daniel;Sanmartin, Carmen
合成了31个新的硒酸酯类化合物，并测定了它们对前列腺癌PC-3细胞的杀伤活性。最有效的化合物还对三个肿瘤细胞系(MCF-7，A-549和HT-29)和一个非肿瘤前列腺细胞系(RWPE-1)进行了测试。13个化合物对所有被研究的肿瘤细胞都显示出显著的活性，其中一些化合物的活性甚至超过了用作参比药物的依托泊苷和顺铂。由于它们显著的效力和/或选择性，选择了四个类似物(5，21，28和30)，以评估它们与可能的氧化还原调节活性有关的氧化还原性质。化合物30的谷胱甘肽过氧化物酶(GPX)活性较弱，2，2-二苯基-1-苦基肼(DPPH)活性较弱。目前的结果表明，类似物5、21、28和30可能是设计改进的抗肿瘤药物的一个有用的起点。(C)2013年爱思唯尔·马森公司。版权所有。
A series of 31 new selenoesters were synthesized and their cytotoxic activity was evaluated against a prostate cancer cell line (PC-3). The most active compounds were also tested against three tumoural cell lines (MCF-7, A-549 and HT-29) and one non-tumour prostate cell line (RWPE-1). Thirteen compounds showed significant activity towards all tumour cells investigated, and some of them were even more potent than etoposide and cisplatin, which were used as reference drugs. Because of their pronounced potency and/or selectivity, four analogues (5, 21, 28 and 30), were selected in order to assess their redox properties related to a possible redox modulating activity. The glutathione peroxidase (GPx) assay showed slight activity for compound 30 and the 2,2-dipheny1-1-picrylhydrazyl-(DPPH) assay showed a weak activity for compounds 5 and 28. The present results revealed that analogues 5, 21, 28 and 30 might serve as a useful starting point for the design of improved anti-tumour agents. (C) 2013 Elsevier Masson SAS. All rights reserved.