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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 4.

In vitro Growth Inhibitory Effects of RABI compounds with B ring substitution

Structure ID R1 R2 IC50 ± SEM(nM)
LNCaP PC3 PPC1 DU145 A375 WM164 MDA-MB-435 MDA-MB-435/LCC6M DR1
graphic file with name nihms466367t4.jpg 15a Me H 10 ± 1 16 ± 1 13 ± 0.2 26 ± 3 9 ± 2 33 ± 5 16 ± 2 18 ± 2
15b Et H 29 ± 20 25 ± 4 30 ± 8 66 ± 2 28 ± 3 16 ± 3 26 ± 3 33 ± 4
15c Bn H 66 ± 6 72 ± 5 77 ± 2 160 ± 41 104 ± 17 34 ± 7 94 ± 18 156 ± 18
15d n-Pr H 49 ± 10 26 ± 6 10 ± 4 72 ± 13 42 ± 3 14 ± 3 37 ± 2 44 ± 4
15e i-Pr H 62 ± 8 53 ± 9 15 ± 3 114 ± 20 38 ± 4 23 ± 5 18 ± 3 44 ± 4
15f graphic file with name nihms466367t5.jpg H 51 ± 6 56 ± 1 63 ± 4 167 ± 16 135 ± 13 56 ± 13 134 ± 15 161 ± 19
15g graphic file with name nihms466367t6.jpg H 20 ± 5 11 ± 3 8 ± 2 37 ± 6 14 ± 3 6 ± 1 11 ± 3 15 ± 5
15h graphic file with name nihms466367t7.jpg H ND ND ND ND 20 ± 2 8 ± 2 25 ± 3 27 ± 3
17a H Me 938 ± 65 1617 ± 144 860 ± 5 2001 ± 163 1302 ± 106 1897 ± 116 1634 ± 102 1586 ± 104
17b H Et 2029 ± 880 3654 ± 192 2078 ± 90 5079 ± 635 2151 ± 48 5514 ± 35 8795 ± 23 5114 ± 27
17c H n-Pr 3094 ± 330 12360 ± 7566 11410 ± 5918 16350 ± 6724 36977 ± 73 19595 ± 91 30540 ± 103 14270 ± 362

ND: Not Determined