Studies on quinones. Part 41: Synthesis and cytotoxicity of isoquinoline-containing polycyclic quinones

Facultad de Química, Pontificia Universidad Católica de Chile, Casilla 306, Santiago, Chile.
Bioorganic & Medicinal Chemistry (Impact Factor: 2.79). 08/2006; 14(14):5003-11. DOI: 10.1016/j.bmc.2006.03.008
Source: PubMed


In the search for new potentially anticancer drugs, isoquinolinequinone-containing polycyclic compounds have been designed and synthesized through highly regiocontrolled cycloaddition reactions of methyl 1,3-dimethyl-5,8-dioxo-5,8-dihydroisoquinoline-4-carboxylate with polarized 1,3-dienes and a thiazole-o-quinodimethane. The new N-heterocyclic quinones were tested on normal human fibroblasts and four distinct human cancer cell lines. Two of the evaluated compounds displayed significant in vitro activity (IC50: 0.44-5.9 microM) comparable to that of the reference drug etoposide.

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