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. 2017 Nov 28;8(12):1224–1229. doi: 10.1021/acsmedchemlett.7b00239

Table 1. Representative PknA and PknB Enzyme Inhibition (Ki): SAR of 2-Aryl-Substituted Quinazolines.

graphic file with name ml-2017-00239e_0007.jpg

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