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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 3.

Enzyme inhibitory and antiviral activity of E and Z isomers of 14a-c

Ring size Inhibitor structure Ki (nM) IC50 (nM)a
15 graphic file with name nihms-145668-t0025.jpg 0.24 ± 0.07 360
15 graphic file with name nihms-145668-t0026.jpg 0.16 ± 0.04 >1000
14 graphic file with name nihms-145668-t0027.jpg 0.18 ± 0.01 6.6
14 graphic file with name nihms-145668-t0028.jpg 0.9 ± 0.3 2.9
13 graphic file with name nihms-145668-t0029.jpg 0.06 ± 0.01 7
13 graphic file with name nihms-145668-t0030.jpg 0.012 ± 0.004 4.6
a

MT-2 human T-lymphoid cells exposed to HIV-1LAI; Saquinavir and amprenavir exhibited IC50 values of 16 nM and 27 nM, respectively.