. Author manuscript; available in PMC: 2015 Nov 1.

Published in final edited form as: Bioorg Med Chem Lett. 2014 Sep 15;24(21):5081–5085. doi: 10.1016/j.bmcl.2014.09.001

Table 1.

STAT3 and STAT1 Activity of 2-guanidinoquinazolines 11a–d

Compd#	R¹	R²	R³	STAT3 IC₅₀¹¹ (μM)	STAT1 IC₅₀¹¹ (μM)	SI^a (STAT1/STAT3)
11a	OEt	H	H	15.7 ± 5.4	>50	>3
11b	Me	H	H	7.9 ± 2.8	>50	>6
11c	Me	H	Me	0.8 ± 0.6	5.9 ± 0.9	>7
11d	H	OEt	H	20.7 ± 3.0	>50	>2

Selectivity index ratio.