867154-99-2Relevant academic research and scientific papers
Synthesis and antitumor effect in vitro and in vivo of substituted 1,3-dihydroindole-2-ones
Christensen, Mette K.,Erichsen, Kamille D.,Trojel-Hansen, Christina,Tj?rnelund, Jette,Nielsen, S?ren J.,Frydenvang, Karla,Johansen, Tommy N.,Nielsen, Birgitte,Sehested, Maxwell,Jensen, Peter B.,Ikaunieks, Martins,Zaichenko, Andrei,Loza, Einars,Kalvinsh, Ivars,Bj?rkling, Fredrik
supporting information; experimental part, p. 7140 - 7145 (2010/12/25)
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: IC50 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.
DIPHENYL OX-INDOL-2-ON COMPOUNDS AND THEIR USE IN THE TREATMENT OF CANCER
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Page/Page column 47-48, (2010/02/14)
The present invention relates to substituted 3,3-diphenyl-1,3-dihydro-indol-2-one compounds, and the use of such compounds for the preparation of a medicament for the treatment of cancer in a mammal. It is postulated that treatment of cancers in which inh
