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2005
Terpenes
U 0200
26- 116
Synthesis of Argentatin A Derivatives as Growth Inhibitors of Human Cancer Cell
Lines in vitro. — Nine analogues of argentatin A, a cycloartane-type triterpene, are
synthesized and assessed for their ability to inhibit growth in vitro in four human cancer
cell lines. The presence of either a bromine atom or formyl moiety at C-2, cf. (II) and
(V), or a double bond at C-1/C-2, cf. (III), as well as the presence of an isoxazol moiety
fused with ring A, enhances the potency of argentatin A in all cell lines tested [compounds (II), (III), (V) and (VI) are more active than argentatin A, (I)]. Additionally,
adequate crystals of an oxime derivative of (I), suitable for X-ray analysis, permit the
assignment of the correct stereochemistry of (I). — (PARRA-DELGADO, H.;
RAMIREZ-APAN, T.; MARTINEZ-VAZQUEZ*, M.; Bioorg. Med. Chem. Lett. 15
(2005) 4, 1005-1008; Inst. Quim., Univ. Nac. Auton. Mex., Coyoacan, 04510 Mexico,
Mex.; Eng.) — H. Hoennerscheid
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