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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):3783–3805. doi: 10.1021/jm400221d

Table 1.

Synthetic analogs of Library 12 and SAR.

graphic file with name nihms-480671-t0008.jpg

Entry Compound
ID		 R3 IC50 (μM) CT-La
1 1 isopropyl 0.60 ± 0.18 (n=27)
2 12a isobutyl 2.37 ± 0.40 (n=2)
3 12b ethyl 6.04 ± 1.34 (n=3)
4 12c methyl 29.90 ± 3.9 (n=2)
5 12d H No inhibition @ 10 μM
6 12e tert-butyl No inhibition @ 10 μM
7 12f cyclopropyl No inhibition @ 10 μM
a

IC50 values are given as the average of 2 or more determinations; n = number of determinations.