Table 3.

Inhibitory potencies of 2-amino-quinazolinyl-dihydropyridimidones 19a–t

Compd#	R1	R2	R3	R4	R5	STAT3 IC5011 (μM)	STAT1 IC5110 (μM)	SIb (STAT1/STAT3)
19a	Me	H	Me	Me	H	5.0 ± 1.8	12.1 ± 0.9	>2
19b	Me	H	Me	Me	Me	6.4 ± 1.6	>50	>7
19c	Me	H	Me	Me	Allyl	14.3 ± 0.9	>50	>3
19d	Me	H	Me	Ph	H	11.2 ± 2.1	>50	>4
19e	OEt	H	H	Me	H	>50	>50	–
19f	OEt	H	H	Me	Me	11.7 ± 5.7	>50	>4
19g	OEt	H	H	Ph	H	3.4 ± 0.6	>50	>14
19h	OEt	H	H	Me	Bn	2.7 ± 2.5	>50	>18
19i	OMe	H	H	Me	H	34.9 ± 2.7	>50	>1
19j	OMe	H	H	Me	Bn	34.7a	50	>1
19k	H	Me	H	Me	H	19.1 ± 1.3	39.7 ± 1.6	>1
19l	H	Me	H	Me	Me	10.5 ± 0.2	35.2 ± 1.1	>3
19m	Me	Me	H	Me	H	24.7 ± 0.5	>50	>2
19n	Me	Me	H	Me	Me	10.4 ± 1.3	>50	>4
19o	−OCH2O−		H	Me	H	>50	>50	–
19p	−OCH2O−		H	Me	Me	>50	>50	–
19q	−OCH2O−		H	Ph	H	13.0 ± 1.4	>50	>3
19r	−OCH2O−		H	Me	Bn	>50	>50	–
19t	H	OMe	H	Me	H	33.9 ± 1.8	>50	>1

^aResults from a single experiment.

^bSelectivity index ratio.