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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 6.

SAR of the para-position substituent at the tail group

graphic file with name nihms-1869382-t0080.jpg
Compound R PfPK6 IC50 (nM)a Pf3D7 blood stage EC50 (nM)b
41 graphic file with name nihms-1869382-t0081.jpg 13 ± 0.5 580 ± 65
59 graphic file with name nihms-1869382-t0082.jpg 390 ± 30 630 ± 13
60 graphic file with name nihms-1869382-t0083.jpg 135 ± 8 Inactivec
61 graphic file with name nihms-1869382-t0084.jpg 310 ± 13 250 ± 7
62 graphic file with name nihms-1869382-t0085.jpg 220 ± 40 270 ± 41
63 graphic file with name nihms-1869382-t0086.jpg 138 ± 14 320 ± 13
64 graphic file with name nihms-1869382-t0087.jpg 26 ± 2 330 ± 11
65 graphic file with name nihms-1869382-t0088.jpg 150 ± 30 660 ± 15
66 graphic file with name nihms-1869382-t0089.jpg 17 ± 3 330 ± 5
67 graphic file with name nihms-1869382-t0090.jpg 13 ± 0.9 160 ± 2
68 graphic file with name nihms-1869382-t0091.jpg 29 ± 3 140 ± 4
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

No inhibition when tested in triplicate at a single concentration of 1 μM.