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基于邻氨基苯甲酸的二酰胺衍生物，引入芳基异噁唑啉药效团作为潜在的抗癌剂：设计、合成与生物评价。

Anthranilic acid-based diamides derivatives incorporating aryl-isoxazoline pharmacophore as potential anticancer agents: design, synthesis and biological evaluation.

机构信息

National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, No. 8, Nanhu Avenue, Wuhan 430064, PR China.

出版信息

Eur J Med Chem. 2012 Aug;54:549-56. doi: 10.1016/j.ejmech.2012.06.001. Epub 2012 Jun 12.

DOI:10.1016/j.ejmech.2012.06.001
PMID:22727445
Abstract

A series of novel anthranilic diamides derivatives containing aryl-isoxazoline moiety were designed and synthesized as a part of our ongoing search for potential anticancer agents. Their structures were confirmed by (1)H NMR, (13)C NMR and ESI-MS analyses. The preliminary assays showed that some of the compounds displayed moderate to good antitumor activities against human lung cancer (NCI-H460), hepatocellular liver carcinoma (HepG2), gastric cancer (SGC-7901 and BGC-823) and breast epithelial adenocarcinoma (MCF-7) cell lines at μM level, which might be developed as novel lead scaffold for potential anticancer agents.

摘要

作为我们正在进行的寻找潜在抗癌剂的一部分，设计并合成了一系列含有芳基异恶唑啉部分的新型邻苯二甲酰亚胺二酰胺衍生物。它们的结构通过（1）H NMR、（13）C NMR 和 ESI-MS 分析得到确认。初步试验表明，一些化合物在 μM 水平上对人肺癌（NCI-H460）、肝癌（HepG2）、胃癌（SGC-7901 和 BGC-823）和乳腺上皮腺癌（MCF-7）细胞系显示出中等至良好的抗肿瘤活性，可能作为潜在抗癌剂的新型先导骨架得到发展。

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