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. Author manuscript; available in PMC: 2017 Jun 15.
Published in final edited form as: Bioorg Med Chem Lett. 2016 Apr 19;26(12):2907–2911. doi: 10.1016/j.bmcl.2016.04.045

Table 1.

IC50 values of heteroaromatic substitution at R3.

graphic file with name nihms783618t1.jpg
Cmpd. R3 R2 Asex.
IC50
(µM)		 Gamet.
IC50
(µM)		 HepG2
IC50
(µM)
11 graphic file with name nihms783618t2.jpg H 0.091 0.097 3.11
12 Me 0.007 0.028 2.60
13 Et 0.183 0.205 3.68
14 graphic file with name nihms783618t3.jpg H 2.82 11.4 2.25
15 Me 0.095 0.236 10.3
16 graphic file with name nihms783618t4.jpg H 0.313 1.14 1.50
17 Me 0.093 0.359 1.73
18 graphic file with name nihms783618t5.jpg H 0.18 0.32 >45.0
19 Me 0.021 0.081 14.5
20 graphic file with name nihms783618t6.jpg H 0.213 0.45 2.54
21 Me 0.017 0.052 1.33
22 graphic file with name nihms783618t7.jpg H 0.081 0.186 >45.0
23 Me 0.025 0.042 3.98
24 graphic file with name nihms783618t8.jpg H 0.412 4.63 >45.0
25 Me 0.158 0.294 23.5
26 graphic file with name nihms783618t9.jpg H 15.4 2.35 >45.0
27 Me 5.78 5.27 31.6
28 graphic file with name nihms783618t10.jpg H 0.214 0.347 3.24
29 Me 0.065 0.157 2.63
30 graphic file with name nihms783618t11.jpg H 5.03 7.46 >45.0
31 Me 17.0 3.64 >45.0