Development of Small Molecular Proteasome Inhibitors Using a Caenorhabditis elegans Screen

Table 1

N-t-BOC and N-benzyl 3-hydroxypyrrolidine analogs prepared.

Compound					EC50 (mM)
	R1	Q1	R2	Q2
1	SO2CH3	t-BOC			N/A
2	SO2(4-CH3C6H4)	t-BOC			141.7
3		t-BOC			13.7
4		t-BOC			15.3
5		t-BOC			N/A
6		t-BOC			73.0
7		t-BOC			114.6
8		Bz			9.0
9		Bz			5.1
10		Bz			N/A
11			SO2CH3	t-BOC	N/A
12				t-BOC	N/A
13				t-BOC	N/A
14				t-BOC	87.1
15				t-BOC	52.4
16				Bz	7.3
Epoxomicin					0.6
Omuralide					47