维尔斯迈尔试剂、硒氢化钠与双氯芬酰氯：新型具有强效抗癌活性的硒代吲哚啉酮的一锅法合成
Vilsmeier reagent, NaHSe and diclofenac acid chloride: one-pot synthesis of a novel selenoindolinone with potent anticancer activity.
作者信息
Ruberte Ana Carolina, Aydillo Carlos, Sharma Arun K, Sanmartín Carmen, Plano Daniel
机构信息
Universidad de Navarra, Facultad de Farmacia y Nutrición, Departamento de Tecnología y Química Farmacéuticas Irunla-rrea 1 E-31008 Pamplona Spain
Instituto de Investigación Sanitaria de Navarra (IdiSNA) Irunlarrea, 3 31008 Pamplona Spain.
出版信息
RSC Adv. 2020 Oct 19;10(63):38404-38408. doi: 10.1039/d0ra07332f. eCollection 2020 Oct 15.
An effective and straightforward synthesis of 3-seleno functionalized indolinone (5) involving Vilsmeier reagent is presented. Likewise, a procedure to achieve lactamization of diclofenac with excellent yields by using hydrides is also ascertained. Compound 5 exhibited impressive growth inhibition in most of the cell lines in an NCI-60 panel, particularly towards resistant breast cancer cells.
本文介绍了一种使用Vilsmeier试剂高效直接合成3-硒官能化吲哚啉酮（5）的方法。同样，也确定了一种使用氢化物以优异产率实现双氯芬酸内酰胺化的方法。化合物5在NCI-60细胞系的大多数细胞系中表现出显著的生长抑制作用，尤其是对耐药乳腺癌细胞。
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