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. 2011 Feb 28;2(4):320–324. doi: 10.1021/ml200004g

Table 1. Substitution at the 4-Position of Aniline SARa.

graphic file with name ml-2011-00004g_0003.jpg

    IC50 (nM)
compd R ACHN HT-29
4a H 10000 (1) 1300 (1)
4b Me 1300 (2) 110 (2)
4c Et 185 (3) 27 (3)
4d Pr 2100 (2) 230 (2)
4e cPr 290 (2) 39 (2)
4f vinyl 104 (3) 15 (3)
4g C≡CH (ethynyl) 42 (2) 5.9 (2)
4h C≡C−Me >3000 (1) >1000 (1)
4i CN >10000 (1) 1600 (1)
4j F >3000 (1) >1000 (1)
4k Cl 4600 (2) 102 (2)
4l Br 325 (4) 15 (4)
4m I 13 (2) 1.5 (2)
a

Numbers in parentheses represent numbers of determinations.