Identification of a C3'-nitrile nucleoside analogue inhibitor of pancreatic cancer cell line growth.

Marc-Olivier Labbé, Laura Collins, Carole-Anne Lefebvre, Wael Maharsy,Janie Beauregard,Starr Dostie,Michel Prévost,Mona Nemer,Yvan Guindon

Bioorganic & medicinal chemistry letters(2020)

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摘要
A synthetic strategy to access a novel family of nucleoside analogues bearing a C3'-nitrile substituted all-carbon quaternary center is presented herein. These purine bearing scaffolds were tested in two pancreatic cancer cell lines harboring either wild-type (BxPC3) or G12V KRAS (Capan2) mutations. A promising compound was shown to have significantly greater efficacy in the Capan2 cell line as compared to Gemcitabine, the clinical gold standard used to treat pancreatic cancer.
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