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2004
Terpenes
U 0200
52- 162
Synthetic and Structure—Activity Relationships of Andrographolide Analogues
as Novel Cytotoxic Agents. — The structural features of andrographolide, a diterpenoidal constituent of A. paniculata, are modified to develop promising anticancer molecules. The in vitro cytotoxic activity of andrographolide and its analogues against different cancer cell lines indicate that i) the intact α-alkylidene γ-butyrolactone moiety
of andrographolide, ii) the ∆12(13) double bond, iii) the C-14 hydroxyl or its ester moiety,
and iv) the ∆8(17) double bond or epoxy moiety are responsible for the cytotoxic activity.
Furthermore, compounds exhibiting good in vitro cytotoxic activity are evaluated for
their in vivo antitumor activity. Of these derivatives, (IX) is the most potent compound
displaying superior activity compared to both the parent andrographolide (I) and epoxide derivative (II). — (NANDRUI*, S.; et al.; Bioorg. Med. Chem. Lett. 14 (2004)
18, 4711-4717; Discovery Chem., Dr. Reddy's Res. Found., Hyderabad 500 050, India;
Eng.) — H. Hoennerscheid
2004
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