Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, UK.
Eur J Med Chem. 2010 Oct;45(10):4523-30. doi: 10.1016/j.ejmech.2010.07.012. Epub 2010 Jul 21.
A series of new indole-based 3,5-disubstituted 1,2,4-oxadiazoles has been designed and synthesised as potential pro-apoptotic antitumour agents, via the base-catalysed condensation reaction between substituted amidoximes and indole esters. Evaluation of antiproliferative activity against the human cancer cell lines COLO 320 (colorectal) and MIA PACA-2 (pancreatic) revealed IC(50) values in the low micromolar range. Selected compounds were able to trigger apoptosis in sensitive cell lines, for example via activation of caspase-3/7, demonstrating that indole-based oxadiazoles possess in vitro antitumour and pro-apoptotic activity.
一系列新型吲哚基 3,5-二取代 1,2,4-噁二唑类化合物被设计并通过取代的偕胺肟与吲哚酯之间的碱催化缩合反应合成，作为潜在的促凋亡抗肿瘤药物。对人类癌细胞系 COLO 320（结肠）和 MIA PACA-2（胰腺）的抗增殖活性评估显示，IC50 值在低微摩尔范围内。选定的化合物能够在敏感细胞系中诱导细胞凋亡，例如通过激活 caspase-3/7，证明基于吲哚的噁二唑类化合物具有体外抗肿瘤和促凋亡活性。
