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. Author manuscript; available in PMC: 2016 Jan 1.
Published in final edited form as: ChemMedChem. 2014 Oct 21;10(1):107–115. doi: 10.1002/cmdc.201402358

Table 1.

Enzymatic inhibitory and antiviral activity of difluoro-bis-THF-derived inhibitors

Entry Inhibitor Ki(nM) IC50(μM)ab
1. graphic file with name nihms684474t1.jpg
3 		0.022 0.0008
2. graphic file with name nihms684474t2.jpg
4 		0.0058 0.0031
3. graphic file with name nihms684474t3.jpg
19 		0.21 0.02
4. graphic file with name nihms684474t4.jpg
20 		3.9 0.64
5. graphic file with name nihms684474t5.jpg
21 		5.14 >1.0
a

Ki values represents at least 5 data points. Standard error in all cases less than 7%. Darunavir exhibited Ki = 16 pM.

b

Values are means of at least three experiments.

c

Human T-lymphoid (MT-2) cells were exposed to 100 TCID50 values of HIV-1LAI and cultured in the presence of each PI, and IC50 values were determined using the MTT assay. Standard error in all cases less than 5%. Darunavir exhibited IC50 = 1.6 nM.