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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.

DOI:10.1039/d0ra07332f
PMID:35517563
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9057275/
Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57ef/9057275/18d55c1f1f1f/d0ra07332f-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57ef/9057275/0bc1ceaa2049/d0ra07332f-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57ef/9057275/4901b25004b9/d0ra07332f-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57ef/9057275/312a677f66a8/d0ra07332f-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57ef/9057275/51e074b20775/d0ra07332f-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57ef/9057275/18d55c1f1f1f/d0ra07332f-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57ef/9057275/0bc1ceaa2049/d0ra07332f-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57ef/9057275/4901b25004b9/d0ra07332f-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57ef/9057275/312a677f66a8/d0ra07332f-f1.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57ef/9057275/18d55c1f1f1f/d0ra07332f-f2.jpg

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