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. Author manuscript; available in PMC: 2009 Dec 23.
Published in final edited form as: Org Biomol Chem. 2008 Aug 11;6(20):3703–3713. doi: 10.1039/b809178a

Table 1.

Enzymatic inhibitory activity of compounds 2,3, and 26–30 and antiviral activity of selected inhibitors against HIV-1LAI

Entry Inhibitor Ki/nMa IC50/μMb
1 graphic file with name nihms151196t1.jpg
2 		0.11 ± 0.01 0.0038 ± 0.0001
2 graphic file with name nihms151196t2.jpg
26 		0.40 ± 0.04 nd
3 graphic file with name nihms151196t3.jpg
27 		5.4 ± 0.22 >1
4 graphic file with name nihms151196t4.jpg
28 		0.51 ± 0.01 0.38 ± 0.02
5 graphic file with name nihms151196t5.jpg
3 		0.18 ± 0.03 0.21 ± 0.04
6 graphic file with name nihms151196t6.jpg
29 		0.50 ± 0.04 nd
7 graphic file with name nihms151196t7.jpg
30 		0.34 ± 0.07 0.0077 ± 0.003
a

Values are means of at least two experiments.

b

MT-2 human T-lymphoid cells exposed to HIV-1LAI ; antiviral activity of amprenavir (APV), saquinavir (SQV) and indinavir (IDV) were 0.03 μM, 0.02 μM and 0.03 μM respectively in this assay. nd: not determined.