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. Author manuscript; available in PMC: 2014 May 15.
Published in final edited form as: Bioorg Med Chem Lett. 2013 Mar 13;23(10):3034–3038. doi: 10.1016/j.bmcl.2013.03.019

Table 1.

Initial phenylthiophene SAR vs. aPKCζa

graphic file with name nihms456317u1.jpg
No. Str. R2 or XR3 Inh (%)a
123 A NH2 100
2 A H 3
3 A NHMe 32
4 A NMe2 60
5 A NHCONH2 14
6 B O-i-Pr 100
7 B graphic file with name nihms456317t1.jpg 57
8 B graphic file with name nihms456317t2.jpg 49
9 B OPh 48
10 B OCH2Ph 100
11 B OCH2Ph-2-Me 64
12 B OCH2Ph-3-Me 67
13 B OCH2Ph-4-Me 50
14 B OCH2Ph-3-OMe 100
15 B OCH2Ph-2-F 100
16 B OCH2Ph-4-F 2
17 B OCH2Ph-3-CN 70
18 B OCH2Ph-4-CN 10
19 B OCH2-4-pyridyl 53
20 B NHEt 50
21 B graphic file with name nihms456317t3.jpg 55
22 B NHCH2Ph 43
23 B NHCH2-4-pyridyl 3
24a24 B COXR3 = CN 87
24b B COXR3 = CO2H 65
a

Inhibition determined from ADP Quest assay with 30 μM of inhibitor using aPKCζ (500 ng/ml). Values are the mean of at least n≥5 and were repeated in independent experiments. Standard error of the mean <20%. The experimental conditions are reported in the Supplementary Material.

Str. = chemical structure.