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3-(6-苯基咪唑并[2,1-][1,3,4]噻二唑-2-基)-1-吲哚衍生物作为治疗胰腺导管腺癌的新型抗癌药物。

3-(6-Phenylimidazo [2,1-][1,3,4]thiadiazol-2-yl)-1-Indole Derivatives as New Anticancer Agents in the Treatment of Pancreatic Ductal Adenocarcinoma.

机构信息

Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF),Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy.

Department of Medical Oncology, VU University Medical Center, Cancer Center Amsterdam, DeBoelelaan 1117, 1081HV Amsterdam, The Netherlands.

出版信息

Molecules. 2020 Jan 14;25(2):329. doi: 10.3390/molecules25020329.

Abstract

A new series of imidazo[2,1-][1,3,4]thiadiazole derivatives was efficiently synthesized and screened for their antiproliferative activity on a panel of pancreatic ductal adenocarcinoma (PDAC) cells, including SUIT-2, Capan-1 and Panc-1. Compounds and , showed relevant antiproliferative activity on all three pre-clinical models with half maximal inhibitory concentration (IC) ranging from 5.11 to 10.8 µM, while the compounds and were active in at least one cell line. In addition, compound significantly inhibited the migration rate of SUIT-2 and Capan-1 cells in the scratch wound-healing assay. In conclusion, our results will support further studies to increase the library of imidazo [2,1-][1,3,4] thiadiazole derivatives for deeper understanding of the relationship between biological activity of the compounds and their structures in the development of new antitumor compounds against pancreatic diseases.

摘要

一系列新型咪唑并[2,1-][1,3,4]噻二唑衍生物被高效合成,并在一组胰腺导管腺癌(PDAC)细胞系上进行了抗增殖活性筛选,包括 SUIT-2、Capan-1 和 Panc-1。化合物和 对所有三种临床前模型均具有相关的抗增殖活性,半数最大抑制浓度(IC)范围为 5.11 至 10.8 µM,而化合物 和 在至少一种细胞系中具有活性。此外,化合物 在划痕愈合试验中显著抑制了 SUIT-2 和 Capan-1 细胞的迁移率。总之,我们的结果将支持进一步的研究,以增加咪唑并[2,1-][1,3,4]噻二唑衍生物库,以加深对化合物生物活性与其结构之间关系的理解,从而开发针对胰腺疾病的新型抗肿瘤化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ad5e/7024338/f9f8535f666e/molecules-25-00329-g001.jpg

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