Retraction of "Design and Synthesis of Novel Cyclic Amine Benzimidazoles for the Treatment of Pancreatic Cancer".

Journal of medicinal chemistry(2017)

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摘要
Wnt/beta-Catenin signaling pathway has a very important role in pancreatic ductal adenocarcinoma (PDAC) initiation and progression. This signaling pathway has been implicated in angiogenesis, maintenance of resistant CICs (cancer-initiating cells), metastasis, regulation of cell cycle, apoptosis and chemoresistance. We investigated the activity of a chemical series of phenyl benzimidazoles, small molecule inhibitors of Wnt signaling in LRP6-expressing HEK 293 cells against PDAC cells. Several benzimidazoles were designed, synthesized and screened under adherent and CIC conditions. Several compounds showed anti-Wnt and cytotoxicity activity in PDAC cells under both conditions, but, in particular, piperidine 43 and pyrrolidine 48 exhibited excellent anti-Wnt activity with IC50 values of 2 nM and potent cytotoxicity activity of IC50 values averaging 1 µM in PDAC cellular assays. Several novel benzimidazole analogs were synthesized and their anti-Wnt and cytotoxicity activity will be described here.
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关键词
novel cyclic amine benzimidazoles,pancreatic cancer”,synthesis
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