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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 5.

SAR of phenylacetylene moiety

graphic file with name nihms-1055475-t0029.jpg
AAK1
enzymatic data		 DENV antiviral activity Cytotoxicity
Cmpd# R AAK1 IC50
(μM)
LanthaScreen		 EC50 (μM) EC90 (μM) CC50 (μM)
21a phenyl 0.209 5.64 10.58 20.1
21b 3-pyridyl 0.00402 1.00 8.12 17.0
21c 3-OCH3-phenyl 0.149 NEa NEa 19.6
21d 4-CH3-phenyl 0.420 7.45 20.5 NEa
21e 4-F-phenyl 0.387 4.21 8.57 19.9
21f 3-CN-phenyl 0.381 10.2 41.2 NEa
a

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