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. Author manuscript; available in PMC: 2012 Dec 27.
Published in final edited form as: Bioorg Med Chem. 2010 Jun 18;18(15):5576–5592. doi: 10.1016/j.bmc.2010.06.038

Table 1.

PI-083 derivatives with moderate activities.

graphic file with name nihms216496t1.jpg
Compound R’ R” In vitro IC50(µM)a
CT-L activity T-L activity PGPH activity
Bortezomib
(Figure 1)		 - - 0.009 ± 0.006 7.0 ± 0.24 0.48 ± 0.021
PI-083 graphic file with name nihms216496t2.jpg H 1.0 ± 0.63 4.5 ± 1.4 4.5 ± 1.2
2s graphic file with name nihms216496t3.jpg H 3.3 ± 0.30 8.15 ± 0.84 14.3 ± 1.60
2h graphic file with name nihms216496t4.jpg H 3.9 ± 0.50 9.25 ± 0.45 21.2 ± 0.79
2f graphic file with name nihms216496t5.jpg H 6.4 ± 0.5 10.7 ± 0.5 13.4 ± 1.1
2d graphic file with name nihms216496t6.jpg H 11.2 ± 3.4 13.2 ± 0.2 16.7 ± 0.5
13h graphic file with name nihms216496t7.jpg OMe 13.7 ± 0.35 24.3 ± 0.04 30 ± 1.5
13j graphic file with name nihms216496t8.jpg OMe 15.3 ± 0.89 23.3 ± 0.94 35 ± 1.90
2b graphic file with name nihms216496t9.jpg H 16.3 ± 6.5 20.65 ± 1.45 25.6 ± 1.39
13e graphic file with name nihms216496t10.jpg H 17 ± 1 24.55 ± 0.55 43.5 ± 2.5
2g graphic file with name nihms216496t11.jpg H 19 ± 0.39 20.9 ± 0.9 50.25 ± 2.25
13d graphic file with name nihms216496t12.jpg H 20.8 ± 0.25 24.65 ± 1.0 49.25 ± 1.75
13c graphic file with name nihms216496t13.jpg H 20.8 ± 0.3 55 ± 2 > 100
a

Tested in triplicate at least twice.