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Indole derivativesR 0140 Synthesis and Bioactivity Evaluation of 3-Hydroxy-3-(phenylethynyl)indol-2-one

Analogues. — Addition of phenylacetylene (I) to isatins (II) in the presence of diethyl-zinc leads to formation of indolones (III) without employing specific zinc reagent lig-ands. The reaction involves activation of the zinc reagent via coordination with carbon-yl substrates that behave "ligand like". Almost all compounds show a protective effect on the apoptosis of PC12 cells, and (IIIf) and (IIIi) exhibit potent in vitro cytotoxicity against lung cancer cell lines. — (CHEN, G.; WANG, Y.; GAO, S.; HE, H.-P.; LI, S.-L.; ZHANG, J.-X.; DING, J.; HAO*, X.-J.; J. Heterocycl. Chem. 46 (2009) 2, 217-220; Lab. Phytochem., Kunming Inst. Bot., Chin. Acad. Sci., Kunming, Yunnan 650204, Peop. Rep. China; Eng.) — H. Hoennerscheid

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