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

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

graphic file with name jm-2010-01212e_0003.jpg

            annexin−S100A10 interaction
 counterscreen
no. R1 R6 R7 R8 X pIC50a IC50 (μM) % controlb
1a CH2CHMeOH H H Me C 4.85 ± 0.09 14 101 ± 7
32 iBu H H Me C <3 >1000  
33 CH2CH2OH H H Me C 4.92 ± 0.16 12 101 ± 6
34 CH2CH2OMe H H Me C 5.12 ± 0.16 8 120 ± 11
35 CH2(CH2)2OMe H H Me C 5.54 ± 0.27 3 111 ± 19
36 CH2CH=CH2 H H Me C 5.19 ± 0.05** 6 105 ± 14
37 CH2CHMeOH H H H C 4.84 ± 0.14 14  
38 CH2CHMeOH H Me H C 4.10 ± 0.10* 79  
39 CH2CHMeOH H H OMe C 3.21 ± 0.35* 616  
40 CH2CHMeOH H OMe H C 5.16 ± 0.05 7 110 ± 3
41 CH2CHMeOH OEt H H C 5.15 ± 0.11 7 112 ± 11
42 CH2CHMeOH H - Me N 3.10 ± 0.01* 794  
43 CH2CHMeOH H H CN C 4.25 ± 0.31 56  
44 CH2CHMeOH H H Cl C 5.57 ± 0.86 3 126 ± 5
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).