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. Author manuscript; available in PMC: 2017 Aug 8.
Published in final edited form as: J Org Chem. 2010 Nov 3;76(1):2–12. doi: 10.1021/jo101638r

Table 4.

IC50 Values for Inhibition of the Human 20S and 26S Proteasome by Salino A Derivatives in a Luminogenic Enzymatic Assaya

IC50
entry compound CT-L activity 20S/26S (nM) C-L activity 20S/26S (nM) T-L activity 20S/26S (nM)
1 rac-cinnabaramide A, (±)−2 2.8±0.6/2.2±0.04 125±12b/230+24b 260±29b/412±83
2 (−)-salino A (1a) (92% ee) 0.8±0.08/2.5±1.3 111±22/156±18 39±7/37±16
3 rac-phenyl deriv.(61) 29±0.7/57±20 788±50/1585±633 702±235/589±120
4 rac-diMePh (63) inact.b,c inact.b,c inact.b,c
5 (−)-homosalino (54) (88% ee) 0.7±0.04/2.3±1.1 144±12/188±3 118±28/125±30
6 velcade 2.6 ±0.7/7.4±1.9 25±7/72±17 254±24/680±150
a

IC50 values are the mean ± standard deviation of 4 or more experiments.

b

The average of 2 experiments.

c

Essentially inactive at >99,000 nM.

(CT-L: chymotrypsin-like activity; C-L: caspase-like activity; T-L: trypsin-like activity)