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2004
Thiazole derivatives
R 0260
Synthesis and Leukemia Cell Growth Inhibition of a Series of 1,3-DithiazolylbenDerivatives. — A slightly modified version of the Hantzsch thiazole synthesis is
52- 109 zene
carried out as a one-pot procedure to furnish the dithiazolylbenzene derivatives (IV)
and (VI). The reaction course can be controlled directing the reaction either to the formation of (IV) or (VI). In the first series, (IVc) inhibits the growth of CEM human leukemia cells at concentrations in the low micromolar range, while in the second series
all congeners show marked cytotoxic effects, especially (VIb) and (VIc). Compounds
(IV) and (VI) are also evaluated for their activity against DNA and RNA viruses as well
as against HIV-1 and HIV-2, but no specific antiviral activity is observed. —
(LAGOJA, I. M.; NAUWELAERTS, K.; BAL-BAHIEU, C.; PASQUALINI, M.;
BAILLY, C.; HERDEWIJN*, P.; Collect. Czech. Chem. Commun. 69 (2004) 7,
1491-1498; Lab. Med. Chem., Rega Inst. Med. Res., Kathol. Univ. Leuven,
B-3000 Leuven, Belg.; Eng.) — H. Hoennerscheid
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