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. Author manuscript; available in PMC: 2018 Nov 22.
Published in final edited form as: J Med Chem. 2017 Nov 9;60(22):9184–9204. doi: 10.1021/acs.jmedchem.7b00941

Table 3.

LDHA Inhibition of analogs 64–68a

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Analog R1 R2 R3 LDHA (w/EDTA)
IC50 ± SD (μM)
64 CONH2 OH 3-Ph 27.7 ± 1.9
65 COOEt CF3 3-Ph >57
66 CH2OH CF3 H 25.5 ± 6.2b
67 tetrazole OH 3-Ph >57
68 CH(OH)CF3 H H >57
a

IC50 values represent the half maximal (50%) inhibitory concentration as determined in the HTS assay (n ≥ 3) using a 22-dose response in 1536-well format.

b

Max. response was less than 50% and thus IC50 values should be considered as lower confidence.