Table 1. Representative PknA and PknB Enzyme Inhibition (Ki): SAR of 2-Aryl-Substituted Quinazolines.
compd | R1 | R2 | PknB Ki (nM) | PknA Ki (nM) |
---|---|---|---|---|
23 | CH2CN | H | 5 | >4000 |
24 | H | CH2CN | 38 | ND |
25 | H | CN | 50 | >4000 |
26 | H | CONH2 | 15 | >4000 |
27 | H | CH2OH | 23 | 2300 |
28 | CH2CONH2 | H | 23 | 1800 |
29 | CONH2 | H | 29 | >4000 |
30 | CN | H | 88 | >4000 |
22 | H | H | 69 | >4000 |
31 | SO2NH2 | H | 24 | 22 |
32 | H | SO2NH2 | 6 | <8 |
33 | <1 | <8 |