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c-KIT enzymatic inhibitory activity and GIST-T1 cell proliferation with the synthesized compounds.
| Compd. | Structure | IC50 (nM) | GI50 (nM) |
|---|---|---|---|
| c-KIT | GIST-T1 | ||
| 81a |
|
82 | 2.2 |
| 81b |
|
97 | 3.2 |
| 81c |
|
20 | 5.4 |
| 81d |
|
98 | 86 |
| 81e |
|
54 | 42 |
| 81f |
|
130 | 25 |
| 81g |
|
43 | 1.0 |
| 90 |
|
82 | 4.9 |
| 93 |
|
38 | 9.9 |
| 95 |
|
50 | 10 |
| 81h |
|
122 | 3.3 |
| 84 |
|
950 | >1000 |
| 81i |
|
86 | 13 |
| 81j |
|
71 | 3.3 |
| 81k |
|
15 | 6.4 |
| Sunitinib |
|
48 | 38 |
