PDF(Pubmed)
Abstract：
Organic isothiocyanates (ITCs) are a class of anticancer agents which naturally result from the enzymatic degradation of glucosinolates produced by Brassica vegetables. Previous studies have demonstrated that the structure of an ITC impacts its potency and mode(s) of anticancer properties, opening the way to preparation and evaluation of synthetic, non-natural ITC analogues. This study describes the preparation of a library of 79 non-natural ITC analogues intended to probe further structure-activity relationships for aryl ITCs and second-generation, functionalized biaryl ITC variants. ITC candidates were subjected to bifurcated evaluation of antiproliferative and antioxidant response element (ARE)-induction capacity against human MCF-7 cells. The results of this study led to the identification of (1) several key structure-activity relationships and (2) lead ITCs demonstrating potent antiproliferative properties.
摘要：
有机异硫氰酸酯(ITC)是一类抗癌剂,其由芸苔属蔬菜产生的芥子油苷的酶促降解天然产生。以前的研究表明，ITC的结构会影响其效能和抗癌特性的模式，为合成的准备和评估开辟了道路，非天然ITC类似物。这项研究描述了79种非天然ITC类似物文库的制备，旨在进一步探索芳基ITC和第二代的结构-活性关系，官能化的联芳基ITC变体。对ITC候选物进行抗增殖和抗氧化反应元件(ARE)对人MCF-7细胞诱导能力的分叉评估。这项研究的结果导致鉴定出（1）几种关键的结构-活性关系和（2）具有有效抗增殖特性的主要ITC。
