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. Author manuscript; available in PMC: 2024 Mar 5.
Published in final edited form as: Eur J Med Chem. 2022 Dec 30;249:115043. doi: 10.1016/j.ejmech.2022.115043

Table 4.

Incorporating CF3 and piperazines to tail group of Ki8751

graphic file with name nihms-1869382-t0070.jpg
Compound R1 R2 R3 R4 PfPK6 IC50 (nM)a Pf3D7 blood stage EC50 (nM)b
Ki8751 H F H F 14 ± 1 n.d.
39 CF3 H H H 0.84 ± 0.04c 540 ± 24
40 CF3 H H F 1.2 ± 0.07c Inactived
41 H graphic file with name nihms-1869382-t0071.jpg H H 13 ± 0.5 580 ± 65
42 H H graphic file with name nihms-1869382-t0072.jpg H 23 ± 1 Inactivee
43 H graphic file with name nihms-1869382-t0073.jpg H H 321 ± 21 Inactivee
44 H H graphic file with name nihms-1869382-t0074.jpg H 68 ± 3 Inactivee
45 CF3 graphic file with name nihms-1869382-t0075.jpg H H 1.9 ± 0.1c 110 ± 4
46 CF3 H graphic file with name nihms-1869382-t0076.jpg H 0.81 ± 0.02c 410 ± 23
47 CF3 graphic file with name nihms-1869382-t0077.jpg H H 21 ± 1 Inactivee
48 CF3 H graphic file with name nihms-1869382-t0078.jpg H 0.29 ± 0.02c Inactivee
a

IC50 values were determined using the KinaseSeeker assay with 5-fold dilutions, presented as mean ± s.e.m. values of two experiments performed in duplicate.

b

EC50 values were determined using the SYBR Green I-based assay with 2-fold dilutions, presented as mean ± s.e.m. values performed in triplicate.

c

IC50 values approach the kinase concentration in the assay. IC50s < 5 nM treated as equipotent.

d

No inhibition when tested up to 5 μM in two experiments, testing in dose-response manner.

e

No inhibition when tested in triplicate at a single concentration of 1 μM. n.d. = not determined.