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. Author manuscript; available in PMC: 2014 May 23.
Published in final edited form as: J Med Chem. 2013 May 13;56(10):4028–4043. doi: 10.1021/jm400241j

Table 1.

SAR of phenyl ring of 1 for CpIMPDH inhibition.

graphic file with name nihms479334u1.jpg
ID R1 IC50 (nM)
(−) BSA (+) BSA
1 2,4-di-ClPh 44 ± 8 120 ± 10
41 2-ClPh 19 ± 2 50 ± 10
42 4-ClPh 105 ± 17 118 ± 3
43 Ph 40 ± 5 50 ± 20
44 4-OMePh 28 ± 2 34 ± 5
45 3-ClPh 20 ± 7 32 ± 8
46 2,3-di-ClPh 3 ± 1 11 ± 1
47 2,6-di-ClPh >5000* n.d
48 1-naphthyl 9 ± 3 14 ± 6
49 1-(4-Cl-naphthyl) 27 ± 1 53 ± 9
*

One determination, n.d. = not determined.