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. Author manuscript; available in PMC: 2018 Mar 10.
Published in final edited form as: ACS Infect Dis. 2017 Feb 8;3(3):225–236. doi: 10.1021/acsinfecdis.6b00202

Table 4.

Activity of linker analogs of 1 against T brucei

graphic file with name nihms847773t12.jpg
Compound R1 R2 T. brucei
EC50 (nM)a 		MRC5-SV2
TC50 (µM)b 		Selectivity
(TC50/EC50)
48a graphic file with name nihms847773t13.jpg H 5.0 26c 5200
48b graphic file with name nihms847773t14.jpg H 5.0 11 2200
48c graphic file with name nihms847773t15.jpg H 980 22 22
48d graphic file with name nihms847773t16.jpg CH3 2200 10 4.5
48e graphic file with name nihms847773t17.jpg H 420 25 60
48f graphic file with name nihms847773t18.jpg H 960 21 22
48g graphic file with name nihms847773t19.jpg H 5500 23 4.2
48h graphic file with name nihms847773t20.jpg H 680 14 21
48i graphic file with name nihms847773t21.jpg H 340 17 50
48j graphic file with name nihms847773t22.jpg H 400 12 30
48k graphic file with name nihms847773t23.jpg H >5000 50 --
a

SD <0.55.

b

SD <3.0 unless otherwise noted.

c

SD=8.8