1. 天然物と医薬品開発

1.
natural products
1.1.
natural product chemistry
1.1.
pharmacophore
biologically active subatances
bioactive substances
physiologically active substances
pharmacologically active substances
1.2.
1-1.
p. 2
1-2.
p. 3
1.3.
1-1. 1981/1 2010/12
S*/NM
(9%)
6%
1,355
15%
S* (4%)
4.7%
S/NM
(11%)
S (29%)
22%
D. J. Newman & G. M. Cragg J. Nat. Prod. 2012, 75, 311.
1-2. 1981/1 2010/12
S*/NM (11%)
1,073
6%
S* (5%)
28%
S/NM
(14%)
36%
D. J. Newman & G. M. Cragg J. Nat. Prod. 2012, 75, 311.
800
432,132
2〜3
225
3〜5
180
3〜7
1,000
!
!
77
70
18
97〜01
2〜3
(combinatorial chemistry)
CADD
(computer associated drug design)
Statistically defined chemical space occupied by Combinatorial,
Natural Products and Drugs Feher M & Schmidt JM J. Chem. Inf. Comput. Sci.
43 218 (2003)
!
1-3.
p. 5
1.4.
!
!
!
!
!
O
O
O
O
O
O
O
OH
H
OH
H
O
Glc O
O
H
vernonioside B1
vernodalin
1g
vernodalin
vernonioside B1
mg
2.81
0.61
0.32
1.64
0.02
0.75
（
）
5%
0
!
9
!
7
!
2
1
!
2
13
0
4
20
20
80%
2
OH
OH
OH
OH
OH
OH
HO
H
10% !
OH
H
OH
HO
1
OH
H
OH OH
OH
H
OH
OH
2
OH O
O
NaO3SO
H
NaO3SO
O
(1β)
D-Qui I-(3
3
1β)-D-Qui II-(4 1β)-D-Glc
(2 1β)
(2
D-Fuc
D-Qui III
H
O
(1β)
I-(3
D-Qui
1β)
1β)-D-Xyl-(4 1β)-D-Glc-(4 1β)-D-Gal
(2 1β)
(2 1β)
D-Fuc
D-Qui II
4
OH
O
NaO3SO
H
O
(1β)
I-(3
D-Qui
1β)-D-Xyl-(4 1β)-D-Glc
(2 1β)
(2 1β)
D-Fuc I-(3 1β)-D-Fuc II
5 D-Qui II
Qui =
Glc =
Fuc =
Xyl =
Gal =
�
12
NMe2
Me 2N
NMe 2
8
11
NMe2
7
MeS
6
1
MeO 4
S
SMe
S
OMe
2
10
S
MeO
S
OMe
MeO
MeO
SMe
S
MeS
MeO
9
MeO
NMe 2
MeO
SMe
Lissoclibadin 1
OMe
S S
NMe2
Lissoclibadin 2
OMe
MeO
S
MeS
S
SMe
OMe
OMe
NMe2
Lissoclibadin 3

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