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. Author manuscript; available in PMC: 2012 Jan 27.
Published in final edited form as: J Med Chem. 2010 Dec 31;54(2):622–634. doi: 10.1021/jm1012787

Table 1.

Enzymatic Inhibitory and Antiviral Activity of Compounds 35a–g, 36, and 37.

Entry Inhibitor Ki (nM) IC50 (μM)a
1 graphic file with name nihms261883t1.jpg
35a 		0.0027 0.0005
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35b 		0.068 0.019
3 graphic file with name nihms261883t3.jpg
35c 		0.005 0.008
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35d 		1.43 --
5 graphic file with name nihms261883t5.jpg
35e 		9 >1 μM
6 graphic file with name nihms261883t6.jpg
35f 		5.3 >1 μM
7 graphic file with name nihms261883t7.jpg
35g 		0.11 --
8 graphic file with name nihms261883t8.jpg
36 		0.010 0.0065
9 graphic file with name nihms261883t9.jpg
37 		0.085 0.0045
a

Values are means of at least two experiments.

b

Human T-lymphoid (MT-2) cells (2 × 103) were exposed to 100 TCID50s of HIV-1LAI and cultured in the presence of each PI, and IC50 values were determined using the MTT assay. The IC50 values of amprenavir (APV), saquinavir (SQV), and indinavir (IDV) were 0.03 μM, 0.015 μM, and 0.03 μM, respectively.