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Identification of a C3'-nitrile nucleoside analogue inhibitor of pancreatic cancer cell line growth.
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-01-21 , DOI: 10.1016/j.bmcl.2020.126983
Marc-Olivier Labbé 1 , Laura Collins 2 , Carole-Anne Lefebvre 3 , Wael Maharsy 2 , Janie Beauregard 2 , Starr Dostie 3 , Michel Prévost 3 , Mona Nemer 2 , Yvan Guindon 4
Affiliation  

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.

中文翻译:

鉴定胰腺癌细胞系生长的C3'-腈核苷类似物抑制剂。

本文提出了一种合成策略,该策略可访问带有C3'-腈取代的全碳四元中心的核苷类似物新家族。这些带有嘌呤的支架在两个具有野生型(BxPC3)或G12V KRAS(Capan2)突变的胰腺癌细胞系中进行了测试。与吉西他滨(一种用于治疗胰腺癌的临床金标准)相比,一种有希望的化合物在Capan2细胞系中具有显着更高的疗效。
更新日期:2020-01-22
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