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. 2012 Jan 16;55(4):1511–1525. doi: 10.1021/jm201195m

Table 1. Heteroatom Analogues of STLCa.

graphic file with name jm-2011-01195m_0001.jpg

compd X R inhibition of basal ATPase activity, Kiapp (nM) ligand efficiency K562 cells, GI50 (nM)
1 (STLC) S (R)-CO2H 135.9 ± 20.5 0.36 1452 ± 76
2 S H 245.5 ± 51.2 0.39 2286 ± 213
6 O H 2157.6 ± 342.2 0.34 nd
7 NH (S)-CO2H 3018.5 ± 398.5 0.29 nd
8 NH H 2659.4 ± 295.6 0.33 nd
rac-9 CH2 CO2H 311.6 ± 53.9 0.34 865 ± 131
(S)-9 CH2 (S)-CO2H 416.5 ± 64.2 0.33 2065 ± 168
(R)-9 CH2 (R)-CO2H 173.5 ± 24.5 0.35 776 ± 26
10 CH2 H 214.7 ± 30.1 0.40 577 ± 61
a

nd = not determined.