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. Author manuscript; available in PMC: 2011 Sep 25.
Published in final edited form as: Bioorg Med Chem Lett. 2009 Dec 5;20(3):1241–1246. doi: 10.1016/j.bmcl.2009.11.123

Table 1.

Enzymatic inhibitory and antiviral activity of allophenylnorstatine-derived inhibitors

Entry Inhibitor Kj(nM) IC50(μM)a,b
1. graphic file with name nihms163721t1.jpg
3a 		0.21 0.02
2. graphic file with name nihms163721t2.jpg
14a 		86.2 nt
3. graphic file with name nihms163721t3.jpg
3b (GRL-0355)		 0.0052 0.009
4. graphic file with name nihms163721t4.jpg
14b 		2.6 nt
5. graphic file with name nihms163721t5.jpg
3c 		0.29 0.013
6. graphic file with name nihms163721t6.jpg
3d 		0.65 nt
7. graphic file with name nihms163721t7.jpg
3e 		0.78 nt
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16a 		2.03 0.051
9. graphic file with name nihms163721t9.jpg
16b 		1.01 0.53
10. graphic file with name nihms163721t10.jpg
16c 		0.31 0.23
a

Values are means of at least three experiments.

b

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. Darunavir exhibited Kj = 16 pM, IC50 = 1.6 nM.