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Short Approach Towards New Isocoumarins and Dihydroisocoumarins and Investigation of their Cytotoxic Activities

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Short Approach Towards New Isocoumarins and Dihydroisocoumarins and Investigation of their Cytotoxic Activities

Isolde Wetzel, Franz Bracher, and J¨urgen Krauss

Department Pharmazie – Zentrum f¨ur Pharmaforschung, Ludwig-Maximilians-Universit¨at M¨unchen, Butenandtstraße 5 – 13, 81377 M¨unchen, Germany

Reprint requests to Dr. J¨urgen Krauss. Fax: +49-89-2180 77171.

E-mail: hjkra@cup.uni-muenchen.de

Z. Naturforsch.2009,64b,313 – 318; received November 25, 2008

3-Substituted isocoumarins were prepared in a short and efficient way from 2-iodobenzoic acid and terminal alkynes in a one-pot Sonogashira reaction. Catalytic hydrogenation gave the corresponding dihydroisocoumarins. The cytotoxic activities of the resulting compounds against human leukaemia cell line (HL 60) were determined in a MTT assay, and structure-activity relationships are discussed.

Key words:Isocoumarin, Dihydroisocoumarin, Sonogashira Reaction, Hydrogenation, Cytotoxic Activity

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