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2004
Benzimidazole derivatives
R 0200
Differential Antiproliferative Activity of New Benzimidazole-4,7-diones. — Ten
such as (II), (IV), and (XII) are prepared to correlate the substi47- 119 benzimidazolediones
tuent effect with the antiproliferative activity on two different tumor cell lines. The
effect of a methoxy or methyl substituent at the quinone ring as well as the shifting of
nitrogen in the pyridine ring from 2- to 3- and 4-positions are examined. Compounds
(IIb), (IVb), and (XII) reveal significant activity on K 562 cells, while (XIIa)—(XIIc)
are active on SW620 cell line. Benzimidazoledione (XIIc) shows highly significant
activity on SW620 cells, comparable to that of doxorubicin. Both the substituents at the
quinone ring as well as the position of the nitrogen in the pyridine moiety are crucial
for activity. — (GARUTI*, L.; ROBERTI, M.; PIZZIRANI, D.; PESSION, A.;
LEONCINI, E.; CENCI, V.; HRELIA, S.; Farmaco 59 (2004) 8, 663-668; Dip. Sci.
Farm., Univ. Bologna, I-40126 Bologna, Italy; Eng.) — H. Hoennerscheid
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