Biomedical Engineering Reference
In-Depth Information
DOX-NH
O
O
O
OMe
O
N
O
N
O
O
O
N
O
O
N
O
HO
O
O
OMe
DOX-NH
14
O
OH
O
OH
OH
DOX-
H
O
O
CH
3
O
O
OH
HO
O
O
O
14a
NH
2
HO
DOX-NH
2
Scheme 10.4
Chemical structure of DOX prodrugs
14
and
14a
[29] .
Figure 10.2
Growth inhibition assay of the
human Molt-3 leukemia cell line, with
addition of prodrugs in the presence and
absence of catalytic antibody 38C2 (cells were
incubated for 72 h): (a) (9) DOX, (b) pro-DOX
14
a, (2) pro - DOX
14
a
+
1
μ
M 38C2, (1)
solvent control; (b) (9) DOX, (b) pro-DOX
14
,
(2) pro - DOX
14
+
1
μ
M 38C2, (1) solvent
control [29] .
circulation half-life. Polyester dendrimers based on bis(HMPA) monomer units
have attracted a lot of attention as they are nonimmunogenic, biodegradable, and
nontoxic in nature. Scheme 10.5 describes the synthesis of a core-functionalized
PEGylated dendrimer [27]. In brief, the tetrafunctional pentaerythritol core
1
was
tailored by benzylidene-protected bis(HMPA) monomer
2
to yield generation
1
dendrimer
3
. The protecting groups were removed by hydrogenolysis, and periph-
