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. Author manuscript; available in PMC: 2020 Jun 27.

Published in final edited form as: J Med Chem. 2019 Jun 12;62(12):5810–5831. doi: 10.1021/acs.jmedchem.9b00136

Table 3.

SAR of the N-acyl moiety

graphic file with name nihms-1055475-t0022.jpg

		AAK1 enzymatic data	DENV antiviral activity		Cytotoxicity
Cmpd#	R	AAK1 IC₅₀ (μM) LanthaScreen	EC₅₀ (μM)	EC₉₀ (μM)	CC₅₀ (μM)
8g	3-pyridyl	0.00432	1.64	7.46	39.7
8i	phenyl	0.108	4.07	50.5	17.3
8j	4-F-phenyl	0.161	8.34	30.2	15.9
8k	4-OCH₃-phenyl	0.0721	NE^a	NE^a	23.6
8l	4-pyridyl	0.381	12.6	26.8	NE^a
8m	benzyl	0.612	142	NE^a	NE^a
8n	cyclopentyl	0.398	3.42	8.34	15.2
8o	cyclohexyl	0.319	4.27	10.8	14.7

^a

NE : No effect (no apparent antiviral effect or effect on cellular viability up to a concentration of 10 μM).