E. Park et al. / Bioorg. Med. Chem. Lett. 22 (2012) 3653–3655
3655
Acknowledgments
O
O
OMe
OH
This work was supported by National Research Foundation of
Korea (No. 2010-0002465) funded by the Ministry of Education,
Science and Technology.
HO
MeO
4e, IC50 = 17.9 µM
4f, IC50 = 90.5 µM
Figure 3. Structures and inhibitory activities of compounds 4e and 4f on b-
hexosaminidase release from RBL-2H3 cells stimulated by DNP–BSA.
Supplementary data
Supplementary data associated with this article can be found,
(IC50 = 88.5
sponding compounds 4a and 4b, showed no activity, even though
at a high concentration (>200 M). Hinokiresinol (1a) and dimeth-
lM). The alcohols 5a and 5b, prepared from the corre-
l
ylhinokiresinol (1b) were relatively less effective than norlignan 4a
for b-hexosaminidase release inhibition. To investigate the effects
of B-ring substituents of 4a, m-hydroxylated derivatives (1c, 4c
and 5c) and m-methoxylated derivatives (1d, 4d and 5d) were
examined for inhibitory activity of b-hexosaminidase release. As
shown in Figure 2, norlignan 4c displayed the most potent activity
References and notes
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In conclusion, we synthesized various norlignans and evaluated
their inhibitory activities against b-hexosaminidase release from
RBL-2H3 cells stimulated by DNP-BSA. In general, the b-vinyl
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