Table 1.

Chemical structures of target compounds and their c-Met inhibitory activities in vitro.

Compound	R	c-Met inhibition
		% Inhibition (10 μΜ)a	IC50 (μM)a
12a	2-F	16.9 ± 3.5	N.D.b
12b	3-F	62.8 ± 1.2	1.2 ± 0.4
12c	4-F	89.2 ± 0.3	0.11 ± 0.02
12d	2-Cl	17.4 ± 3.7	N.D.
12e	3-Cl	54.5 ± 6.9	4.8 ± 0.5
12f	4-Cl	63.8 ± 0.7	0.93 ± 0.10
12g	4-Br	54.2 ± 0.1	5.5 ± 0.9
12h	2-I	21.6 ± 2.5	N.D.
12i	3-I	66.0 ± 0.8	0.54 ± 0.13
12j	2-CH3	23.0 ± 0.4	N.D.
12k	3-CH3	52.7 ± 1.6	8.5 ± 2.0
12l	4-CH3	69.0 ± 1.2	0.32 ± 0.07
12m	4-CH2CH3	95.0 ± 0.3	0.056 ± 0.012
12n	4-C(CH3)3	97.1 ± 3.5	0.030 ± 0.008
12o	2-OCH3	24.2 ± 0.1	N.D.
12p	2,6-di-F	25.9 ± 1.5	N.D.
12q	2,6-di-Cl	37.0 ± 4.0	N.D.
12r	3,4-di-Cl	55.4 ± 2.9	5.3 ± 1.6
12s	2-Br-5-F	23.0 ± 1.1	N.D.
cabozantinibc		N.D.	0.0045 ± 0.0006

^an = 3 (mean ± SD).

^bN.D.: not determined.

^cUsed as a positive control.