Chemistry Reference
In-Depth Information
Table 4.1
IGF-IR biochemical potencies for compounds 1a-l
NH
2
Q
1
N
N
N
R
1
1
.
Q
1
R
1
Compound
IC
50
(mM)
1a
3-BnOC
6
H
4
cyclobutyl
0.606
1b
Ph
cyclobutyl
410.0
1c
3-MeOC
6
H
4
cyclobutyl
410.0
1d
4-MeOC
6
H
4
cyclobutyl
410.0
1e
4-BnOC
6
H
4
cyclobutyl
1.97
1f
4-PhOC
6
H
4
cyclobutyl
410.0
1g
3-BnOC
6
H
4
cyclopentyl
1.05
1h
3-BnOC
6
H
4
phenyl
1.68
1i
3-BnOC
6
H
4
cyclohexyl
3.51
1j
3-BnOC
6
H
4
cycloheptyl
3.79
1k
3-BnOC
6
H
4
H
410.0
1l
3-BnOC
6
H
4
1-naphthyl
410.0
Table 4.2
IGF-IR biochemical potencies for compounds 13a-d
O
R
2
NH
2
N
N
N
13
.
R
2
Compound
IC
50
(mM)
13a
CH
2
-cyclopropyl
2.27
13b
CH
2
-cyclohexyl
1.11
13c
CH
2
-2-pyridyl
1.09
13d
CH
2
-3-pyridyl
410.0
imidazopyrazine ring while maintaining the preferred 3-BnOC
6
H
4
moiety at C1.
A range of substituted C4-cyclohexyl and C3-cyclobutyl analogs were synthe-
sized, specifically, a series of amides and aminomethyl derivatives (Table 4.4).
The trans-(aminomethyl)cyclohexyl derivative 15c displayed biochemical and
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