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. Author manuscript; available in PMC: 2012 Dec 22.
Published in final edited form as: J Med Chem. 2011 Nov 29;54(24):8582–8591. doi: 10.1021/jm201134m

Table 5.

Anti-HIV Activity (EC50) and Average Cytotoxicity (CC50), μM, of Catechol Diether Derivatives and Reference NNRTIs for WT and Viral Variants.

Compd EC50
CC50
WT Y181C K103N/Y181C
20 0.14 21 2.2 77
22 0.090 6.7 1.2 32
25 0.014 0.52 1.7 >100
26 0.013 0.62 1.7 13
27 0.017 0.24 0.57 21
31 0.043 0.92 2.8 59
32 0.020 0.80 >43 >61
40 0.015 0.98 8.0 >90
41 0.005 0.37 1.6 22
42 0.000055 0.049 0.22 10
43 0.0032 0.15 0.90 48
44 0.00032 0.016 0.085 45
45 0.020 2.8 ND 30
nevirapine 0.11 >100 >100 >100
nevirapinea 0.081 >10 >10
efavirenz 0.002 0.010 0.030 15
efavirenza 0.0014 0.002 0.037
etravirine 0.001 0.008 0.005 11
etravirinea 0.001 0.007 0.004
rilpivirine 0.00067 0.00065 0.002 >1
rilpivirinea 0.0004 0.0013 0.001 8
a

Literature data; see ref. 28.