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. 2016 Mar 1;7(5):502–507. doi: 10.1021/acsmedchemlett.6b00039

Table 1. Inhibition Data for DAQ Isomeric Derivatives 3aq and 4aq against Self-Induced Aβ40 and Aβ42 Aggregation.

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  IC50 (μM)a,b
  IC50 (μM)a,b
 
N4-isomer Aβ40 Aβ42 R-group Aβ40 Aβ42 N2-isomer
3a 4.8 >25 benzyl 2.2 8.4 4a
3b 3.6 >25 3-Me-benzyl >25 >25 4b
3c 3.9 >25 4-Me-benzyl 13.1 22.5 4c
3d 20.6 n.a 3-OMe-benzyl >25 >25 4d
3e 1.1 >25 4-OMe-benzyl 6.8 >25 4e
3f 3.5 21.0 3-CF3-benzyl 12.5 13.8 4f
3g 1.9 >25 4-CF3-benzyl 2.3 5.3 4g
3h 1.9 >25 3-Cl-benzyl 5.9 13.4 4h
3i 0.62 >25 4-Cl-benzyl 0.93 8.1 4i
3j 0.58 22.3 3-Br-benzyl 1.5 2.7 4j
3k 0.08 14.8 4-Br-benzyl 1.7 1.7 4k
3l 2.8 >25 3-F-benzyl 11.3 14.7 4l
3m 3.1 >25 4-F-benzyl >25 >25 4m
3n 7.8 >25 phenethyl 14.9 >25 4n
3o 14.9 n.a n-Pr >25 >25 4o
3p 10.2 n.a i-Pr >25 >25 4p
3q 13.6 >25 cyclohexylmethyl >25 >25 4q
DAQ P.A P.A   1.5 3.1 curcumin
orange G 3.0 8.7 2.6 4.1 resveratrol
a

IC50 values are calculated based on the ThT-based fluorescence spectroscopy assay (excitation = 440 nm, emission = 490 nm).

b

Values are mean values of triplicate readings for three independent experiments. n.a = not active. P.A = promotes aggregation.