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. Author manuscript; available in PMC: 2017 Sep 8.
Published in final edited form as: J Med Chem. 2016 Aug 25;59(17):7950–7962. doi: 10.1021/acs.jmedchem.6b00752

Table 2.

Carboxanilide substitution effects at C-4

graphic file with name nihms847875u3.jpg
Cmpd. X ED50(nM)a Cmpd. X EC50(nM)a
10a H 97 10o 2'Cl 1300
10b 3'-Cl, 4'-OMe 53 10p 3'-Cl 162
10c (N-Me) 3'-Cl, 4'-OMe >5000 10q 4'-C 497
10d 3'-CN 50 10r 3'-OCF3 57
10e (cis) 3'-CN 207 10s 4'-OCF3 1022
10f (N-Me) 3'-CN 4115 10t 3'-CF3 136
10g 2'-CN 1426 10u 3'-CN, 4'-OMe 29
10h 4'-CN 1134 10v 3'-CN, 4'-F 19
10i 4'-OMe 65 10w (cis) 3'-CN, 4'-F 146
10j 3'-OMe 190 10x 3'-CN, 4'-Cl 157
10k 2'-OMe 943 10y 3'-CN, 5'-F 58
10l 2'-F 475 10z 3'-CN, 5'-Cl 25
10m 3'-F 89 10aa 3'-CN, 5'-CN 1104
10n 4'-F 56
a

Concentration causing 50% reduction in growth of P falciparum 3D7 co-cultured with human erythrocytes; values shown are from two independent experiments done in triplicate.