Table 1.
|
Compound |
IC50, nM
(L1210)a |
Compound |
IC50, nM
(L1210)a |
|
Natural enantiomers |
Unnatural
enantiomers |
||
|
37, (+)-N-BOC-CPI |
160 (210) |
(-)-N-BOC-CPI |
1000 (1000) |
|
45, (+)-CPI-TMI |
0.007 (0.008) |
(-)-CPI-TMI |
1 (1) |
|
46, (+)-CPI-(5-MeO)indole |
0.009 (0.008) |
(-)-CPI-(5-MeO)indole |
1 (10) |
|
47, (+)-CPI-indole |
0.050 (0.070) |
(-)-CPI-indole |
10 (70) |
|
48, (+)-CPI-indole2 |
0.003 (0.002) |
(-)-CPI-indole2 |
1 (1) |
|
49, (+)-CPI-CDPI1 |
0.009 (0.009) |
(-)-CPI-CDPI1 |
2 (4) |
|
1, (+)-CC-1065 |
0.020 |
(-)-CC-1065 |
0.020 |
|
2, (+)-duocarmycin SA |
0.006 |
(-)-duocarmycin
SA |
0.100 |
|
38, (+)-N-BOC-C7-MeCPI |
330 |
|
|
|
39, (+)-N-BOC-DSA |
6 |
(-)-N-BOC-DSA |
60 |
|
|
O-benzyl derivatives |
|
|
|
40 |
0.1 |
|
50 |
|
41 |
0.1 |
|
50 |
|
42 |
Nd |
|
100 |
|
43 |
0.5 |
|
100 |
|
44 |
1.3 |
|
220 |
a The value in parentheses is the IC50 for the corresponding seco derivatives