Substituted E-3-(2-Chloro-3-indolylmethylene)1,3-dihydroindol-2-ones with Antitumor Activity. Effect on the Cell Cycle and Apoptosis

The synthesis and antitumor activity of new E-3-(2-chloro-3-indolylmethylene)1,3-dihydroindol-2-ones is described. They were studied at the National Cancer Institute, taking into consideration the 50% growth inhibitory power (pGI50), the cytostatic effect (pTGI = total growth inhibition), and the cy...

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Veröffentlicht in:Journal of medicinal chemistry 2007-07, Vol.50 (14), p.3167-3172
Hauptverfasser: Andreani, Aldo, Burnelli, Silvia, Granaiola, Massimiliano, Leoni, Alberto, Locatelli, Alessandra, Morigi, Rita, Rambaldi, Mirella, Varoli, Lucilla, Calonghi, Natalia, Cappadone, Concettina, Farruggia, Giovanna, Zini, Maddalena, Stefanelli, Claudio, Masotti, Lanfranco
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Sprache:eng
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Zusammenfassung:The synthesis and antitumor activity of new E-3-(2-chloro-3-indolylmethylene)1,3-dihydroindol-2-ones is described. They were studied at the National Cancer Institute, taking into consideration the 50% growth inhibitory power (pGI50), the cytostatic effect (pTGI = total growth inhibition), and the cytotoxic effect (pLC50). All the compounds were potent growth inhibitors, with mean pGI50 ranging from 5.26 to 7.72. They were also analyzed with NCI COMPARE algorithm. Further studies were dedicated to the effects on the cell cycle and apoptosis.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm070235m