Development of new deoxycytidine kinase inhibitors and noninvasive in vivo evaluation using positron emission tomography

JM Murphy, AL Armijo, J Nomme, CH Lee…

文献索引：Murphy, Jennifer M.; Armijo, Amanda L.; Nomme, Julian; Lee, Chi Hang; Smith, Quentin A.; Li, Zheng; Campbell, Dean O.; Liao, Hsiang-I.; Nathanson, David A.; Austin, Wayne R.; Lee, Jason T.; Darvish, Ryan; Wei, Liu; Wang, Jue; Su, Ying; Damoiseaux, Robert; Sadeghi, Saman; Phelps, Michael E.; Herschman, Harvey R.; Czernin, Johannes; Alexandrova, Anastassia N.; Jung, Michael E.; Lavie, Arnon; Radu, Caius G. Journal of Medicinal Chemistry, 2013 , vol. 56, # 17 p. 6696 - 6708

全文：HTML全文

被引用次数: 12

摘要

Combined inhibition of ribonucleotide reductase and deoxycytidine kinase (dCK) in multiple cancer cell lines depletes deoxycytidine triphosphate pools leading to DNA replication stress, cell cycle arrest, and apoptosis. Evidence implicating dCK in cancer cell proliferation and survival stimulated our interest in developing small molecule dCK inhibitors. Following a high throughput screen of a diverse chemical library, a structure–activity relationship study ...