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. Author manuscript; available in PMC: 2014 Apr 25.
Published in final edited form as: J Med Chem. 2013 Apr 9;56(8):3318–3329. doi: 10.1021/jm4001117

Table 1.

In vitro Growth Inhibitory Effects of ABI compounds with A ring substitution

Structure ID R1 IC50 ± SEM (nM)
LNCaP PC3 PPC1 DU145 A375 MDA-MB-435 MDA-MB-435/LCC6MDR1 Average IC50
graphic file with name nihms466367t1.jpg 5aa3 H 152 ± 35 288 ± 30 133 ± 6 196 ± 29 160 ± 20 ND ND 186
5da3 Me 12 ± 1 9 ± 0.4 15 ± 1 11 ± 0.1 9 ± 2 5 ± 1 11 ± 2 10
5a Et 9 ± 1 13 ± 1 15 ± 1 25 ± 2 14 ± 5 25 ± 4 27 ± 3 18
5b i-Pr 171 ± 34 136 ± 20 173 ± 0.3 482 ± 40 ND 312 ± 4 250 ± 4 254
5c t-Bu 423 ± 71 436 ± 115 294 ± 2 1698 ± 400 ND 3691 ± 60 3074 ± 50 1603

ND: Not Determined