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 ...

Discovery and synthesis of novel 4-aminopyrrolopyrimidine Ti...

[Arcari, Joel T.; Beebe, Jean S.; Berliner, Martin A.; Bernardo, Vincent; Boehm, Merin; Borzillo, Gary V.; Clark, Tracey; Cohen, Bruce D.; Connell, Richard D.; Frost, Heather N.; Gordon, Deborah A.; Hungerford, William M.; Kakar, Shefali M.; Kanter, Aaron; Keene, Nandell F.; Knauth, Elizabeth A.; Lagreca, Susan D.; Lu, Yong; Martinez-Alsina, Louis; Marx, Matthew A.; Morris, Joel; Patel, Nandini C.; Savage, Doug; Soderstrom, Cathy I.; Thompson, Carl; Tkalcevic, George; Tom, Norma J.; Vajdos, Felix F.; Valentine, James J.; Vincent, Patrick W.; Wessel, Matthew D.; Chen, Jinshan M. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 10 p. 3059 - 3063]