. Author manuscript; available in PMC: 2024 Apr 14.

Published in final edited form as: ACS Infect Dis. 2023 Mar 15;9(4):1004–1021. doi: 10.1021/acsinfecdis.3c00025

Table 1.

Antiplasmodial and Kinase Activities of Compound 1 Structural Analogues


ID	antiplasmodial activity			cytotoxicity		kinase activity
ID	Pf Dd2 EC₅₀ (nM)	Pf 3D7 EC₅₀ (nM)	RI^a	HepG2 EC₅₀ (nM)	SI^b	PLK1 IC₅₀ (nM)
BI-2536 (1)	178 ± 12	135 ± 35	1.3	3730 ± 520	21	0.83
compound 2	432 ± 47	347 ± 52	1.2	>25,000	> 58	>10,000
compound 3	2330 ± 160	1530 ± 250	1.5	3030 ± 200	1.0	204
compound 4	4190 ± 260	3250 ± 550	1.3	8550 ± 720	2.0	430
compound 5	>5000	nt	-	>25,000	-	>10,000
compound 6	>5000	nt	-	6200 ± 470	<1.0	nt
compound 7	1490 ± 260	1540 ± 350	0.97	6390 ± 130	4.0	270
compound 8	2420 ± 440	2350 ± 650	1.0	21,800 ± 700	9.0	6200
compound 9	>5000	nt	-	>25,000	-	8800
compound 10	>5000	nt	-	22,300 ± 1290	<4.0	nt

Resistance Index (RI) = Dd2 EC₅₀/3D7 EC₅₀.

Selectivity Index (SI) = HepG2 EC₅₀/Dd2 EC₅₀.

nt = not tested.

Values shown are the average EC₅₀ ± standard error of the mean (SEM) from at least three biological replicates. Human PLK1 IC₅₀ values were obtained from prior publication or from Selleck Chemicals.^15,16