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. 2020 May 18;11(8):885–895. doi: 10.1039/d0md00057d

Table 4. Additional inhibitors with 2,5-substituted imidazo[1,2-a]pyridine linker.

Inline graphic
Compound number Ar R T. brucei a EC50 (nM) CRL-8155 b CC50 (nM) HepG2 c CC50 (nM)
34 graphic file with name d0md00057d-u37.jpg Cl 1900 ND d ND
35 graphic file with name d0md00057d-u38.jpg Cl 64 16 100 43 200
36 graphic file with name d0md00057d-u39.jpg Cl 196 ND ND
37 graphic file with name d0md00057d-u40.jpg Cl 1780 ND ND
38 graphic file with name d0md00057d-u41.jpg Cl >2000 ND ND
39 graphic file with name d0md00057d-u42.jpg Cl 3.5 ± 0.1 (n = 2) 9500 >50 000
40 graphic file with name d0md00057d-u43.jpg Cl 3.1 ± 0.5 (n = 6) 19 000 28 200
41 graphic file with name d0md00057d-u44.jpg F 59 15 700 >50 000
42 graphic file with name d0md00057d-u45.jpg F 8.4 ± 3.1 (n = 2) 10 400 >50 000
43 graphic file with name d0md00057d-u46.jpg F 7.2 ± 1.7 (n = 4) >25 000 >25 000

aControl for T brucei EC50 assay average ± SEM: pentamidine (2.4 ± 0.3 nM; n = 10).

bControl for CRL-8155 EC50 assay average ± SEM: quinacrine (6.1 ± 0.6 μM; n = 5).

cControl for HepG2 EC50 assay average ± SEM: quinacrine (10.9 ± 1.1 μM; n = 4).

dND: not determined.