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. Author manuscript; available in PMC: 2014 May 1.
Published in final edited form as: Bioorg Med Chem. 2013 Feb 21;21(9):2600–2617. doi: 10.1016/j.bmc.2013.02.023

Table 2. Inhibition of purified recombinant human MetAPs by pyridinylpyrimidine derivatives.

graphic file with name nihms459675u2.jpg
Cmpd R IC50a (μM) IC50 ratio (type 2/1)
HsMetAP1 HsMetAP2
16a graphic file with name nihms459675t4.jpg 0.8 ± 0.1 114 ± 12 143
16b graphic file with name nihms459675t5.jpg 1.1 ± 0.1 >300 >272
18a graphic file with name nihms459675t6.jpg 0.6 ± 0.1 22 ± 4 37
18b graphic file with name nihms459675t7.jpg 1.1 ± 0.2 >300 >272
20a graphic file with name nihms459675t8.jpg 1.4 ± 0.2 108 ± 11 77
20b graphic file with name nihms459675t9.jpg 1.7 ± 0.5 101 ± 12 59
22a graphic file with name nihms459675t10.jpg 1.3 ± 0.5 188 ± 17 145
22b graphic file with name nihms459675t11.jpg 0.8 ± 0.2 197 ± 22 246
24a graphic file with name nihms459675t12.jpg 0.8 ± 0.1 9.4 ± 1.0 12
24b graphic file with name nihms459675t13.jpg 0.6 ± 0.1 95 ± 14 158
a

IC50 values of compounds to inhibit human MetAPs were shown as mean ± SD of three determinations. The bottom values of all inhibitory dose-response curves were smaller than 10%.