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. 2015 Oct 1;25(19):4219–4224. doi: 10.1016/j.bmcl.2015.07.095

Table 2.

Activity of 3-substituted-1-hydroxy-7-phenethyl-3,7-dihydro-1H-purine-2,6-diones 8

Cmpd graphic file with name fx14.gif IC50a (μM) (Caf1) IC50a (μM) (PARN)
8a CH3 9.3 ± 1.7 n.d.
8b CH2(CH2)2Ph 2.1 ± 0.3 n.d.
8c CH2CH3 12.2 ± 3.5 n.d.
8d CH2(CH2)3CH3 4.8 ± 1.2 n.d.
8e graphic file with name fx15.gif 1.7 ± 0.4 n.d.
8f CH2(CH2)7CH3 9.9 ± 3.6 n.d.
8g CH2(CH2)8CH3 20.7 ± 6.7 n.d.
8h CH2(CH2)10CH3 29.5 ± 22.4 n.d.
8i CH2Ph 14.5 ± 0.9 n.d.
8j graphic file with name fx16.gif 0.59 ± 0.11 23.9 ± 3.7
8k graphic file with name fx17.gif 8.7 ± 0.3 n.d.
a

IC50 values were determined using a fluorescence-based biochemical assay as described.22 Also indicated are the standard errors of the means (n = 3). N.d., not determined.