Identification and synthesis of substituted pyrrolo [2, 3-d] pyrimidines as novel firefly luciferase inhibitors
Y Liu, J Fang, H Cai, F Xiao, K Ding, Y Hu
Index: Liu, Yang; Fang, Jianping; Cai, Haiyan; Xiao, Fei; Ding, Kan; Hu, Youhong Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 18 p. 5473 - 5482
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Citation Number: 11
Abstract
A novel firefly luciferase inhibitor (3a) with a pyrrolo [2, 3-d] pyrimidine core was identified in a cell-based NF-κB luciferase reporter gene assay. It potently inhibited the firefly luciferase derived from Photinus pyralis with an IC50 value of 0.36±0.05 μM. Kinetic analysis of 3a inhibition showed that it is predominantly competitive with respect to d-luciferin and uncompetitive with respect to ATP. Therefore, several pyrrolo [2, 3-d] pyrimidine ...
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