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. 2011 Mar 4;54(7):2080–2094. doi: 10.1021/jm101212e

Table 4. Inhibition of the S100A10 Interaction with Annexin A2 by 1,5-Substituted 4-Aroyl-3-hydroxy-1H-pyrrol-2(5H)-ones and Activity in the Counterscreen Assay.

graphic file with name jm-2010-01212e_0004.jpg

              annexin−S100A10 interaction
 counterscreen
no. R1 R3 R6 R7 R8 X pIC50a IC50 (μM) % controlb
45 CH2CH=CH2 H H   H N <3 >1000  
46 CH2CH=CH2 H H   Me N 4.55 ± 0.17 28 102 ± 9
47 CH2CH=CH2 H H H Cl C 5.20 ± 0.06 6 120 ± 6
48 CH2(CH2)2OMe H H   H N <3 >1000  
49 CH2(CH2)2OMe H H   Me N 3.57 ± 0.01* 269  
50 CH2(CH2)2OMe F H   Me N 3.74 ± 0.01* 182  
51 CH2(CH2)2OMe F H H Cl C 3.73 ± 0.42* 186  
52 CH2(CH2)2OMe H OEt H H C 4.97 ± 0.09 11 117 ± 9
53 CH2(CH2)2OMe F OEt H H C 5.31 ± 0.11 5 127 ± 19
a

Data were expressed as % of the specific signal of the nontreated control and analyzed by nonlinear regression using Graphpad Prism. pIC50 ± standard error of the fit (n = 4−8 data points per concentration, 0.4−100 μM). The midpoint of the dose−response curve is given based on a floating fit unless indicated as follows: *, bottom fixed at zero; **, bottom fixed at zero, top fixed at 100%.

b

Percent remaining signal at 50 μM compound relative to diluent only (mean ± standard error mean of >3 determinations).