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Synthesis and antitumor effect in vitro and in vivo of substituted 1,3-dihydroindole-2-ones

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Optimization of the anticancer activity for a class of compounds built on a 1,3-dihydroindole-2-one scaffold was performed. In comparison with recently published derivatives of oxyphenisatin the new analogues exhibited an equally potent antiproliferative activity in vitro and improved tolerability and activity in vivo. The best compounds from this series showed low nanomolar antiproliferative activity toward a series of cancer cell lines (compound (S)-38: IC(50) of 0.48 and 2 nM in MCF-7 (breast) and PC3 (prostate), respectively) and potent antitumor effects in well tolerated doses in xenograft models. The racemic compound (RS)-38 showed complete tumor regression at a dose of 20 mg/kg administered iv on days 1 and 7 in a PC3 rat xenograft.
Original languageEnglish
JournalJournal of Medicinal Chemistry
Volume53
Issue number19
Pages (from-to)7140-5
Number of pages6
ISSN0022-2623
DOIs
Publication statusPublished - 14 Oct 2010

ID: 31055181