. Author manuscript; available in PMC: 2013 Jul 15.

Published in final edited form as: Bioorg Med Chem Lett. 2012 Jun 6;22(14):4579–4584. doi: 10.1016/j.bmcl.2012.05.107

Table 2.

SAR of 3-amino-1H-indazol-benzamides (II)


		Cellular antiproliferative activity (EC₅₀, µM)^a
Compds	Structure	MOLM13 (FLT3)	PDGFRα- T674M-Ba/F₃	Kit-T607I Ba/F₃	wt-Ba/F₃
4		0.005	0.017	0.198	>10
10		0.005	0.031	1.424	>10
11		0.002	0.001	0.177	3.1
12		0.559	0.078	2.908	>10
13		3.426	1.817	1.22	>10
14		0.035	0.927	1.094	2.0
15		<0.001	0.13	-^b	0.12
16		0.033	0.845	5.366	5.3
17		0.004	0.017	3.169	>10
18		<0.001	0.001	1.528	>10
22		0.002	0.001	0.727	4.4

Cellular antiproliferative activity (EC₅₀, µM) on MOLM13, mutant PDGFRα–T674M–Ba/F3, mutant Kit–T670I–Ba/F3 and wt-Ba/F3, values are means of two experiments.

Nonsensical value.