The protein aggregation inhibitor YAT2150 has potent antimalarial activity in Plasmodium falciparum in vitro cultures

Table 2 In vitro antiplasmodial activity in P. falciparum cultures of amyloid pan-inhibitors and β-sheet intercalators

Compound	Chemical family	IC₅₀ in 3D7 strain (µM) ± SEM	IC₅₀ in K1 strain (µM) ± SEM	Selectivity index in vitro¹
HUP5ANTRA^a	Aminoquinoline	0.78 ± 1.86	N/D	97.7
HUP7ANTRA^a	Aminoquinoline	7.53 ± 0.84	N/D	3.9
HUP10ANTRA^a	Aminoquinoline	8.73 ± 1.61	N/D	9.7
HUP7TH	Aminoquinoline	0.13 ± 0.01	0.47 ± 0.36^b	60.0
HUP8TH	Aminoquinoline	0.21 ± 0.01	0.39 ± 0.14^b	23.3
HUP9TH	Aminoquinoline	0.16 ± 0.02	0.35 ± 0.06^b	30.6
HUPH10TH	Aminoquinoline	0.18 ± 0.05	3.50 ± 2.29^b	18.9
HUPNTH	Aminoquinoline	0.31 ± 0.02	0.43 ± 0.22^b	11.0
HUPNTCl	Aminoquinoline	0.15 ± 0.01	0.52 ± 0.13^b	42.0
DP128^c	Aminoquinoline	0.65 ± 0.14	N/D	75.4
DONE3TCl	Aminoquinoline	0.08 ± 0.03	0.36 ± 0.07^c	157.5
YAT2150	Bis(styrylpyridinium) salt	0.09 ± 0.02	N/D	37.8
ThT	Benzothiazolium salt	1.57 ± 0.23	N/D	N/D
Congo Red	Bis(naphthalenesulfonate)	> 15	N/D	N/D

¹50% cytotoxic concentration (CC₅₀)/IC₅₀ in 3D7 strain. See Additional file 1: Table S9 for CC₅₀ values
^a[57]
^b[39]
^c[40]
N/D no data

ISSN: 1741-7007