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. Author manuscript; available in PMC: 2010 Dec 10.
Published in final edited form as: J Med Chem. 2009 Dec 10;52(23):7689–7705. doi: 10.1021/jm900695w

Table 1.

Enzyme inhibitory and antiviral activity of inhibitors 13a-h

graphic file with name nihms-145668-t0009.jpg
Compd m n Ki(nM) IC50(nM)a Ring Size
by RCM
13a 4 4 16.5 ± 0.5 >1000 15
13b 4 3 11.5 ± 0.4 >1000 14
13c 4 2 6.9 ± 0.1 ND 13
13d 4 1 10 ± 2 ND 12
13e 1 4 1.70 ± 0.07 270 12
13f 1 3 1.02 ± 0.08 290 11
13g 1 2 0.63 ± 0.01 ND 10
13h 1 1 0.10 ± 0.01 ND 9
a

human T-lymphoid cells, MT-2 cells (2×103), were exposed to HIV-1LAI (100 TCID50), cultured in the presence of each PI, and IC50 values were determined by using the MTT assay. The IC50 values of saquinaivr (SQV) and amprenavir (APV) tested as reference agents were 16 nM and 27 nM, respectively. ND: not determined.