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

Research output: Contribution to journalJournal articleResearchpeer-review

Standard

Synthesis and antitumor effect in vitro and in vivo of substituted 1,3-dihydroindole-2-ones. / Christensen, Mette Knak; Erichsen, Kamille Dumong; Trojel-Hansen, Christina; Tjørnelund, Jette; Nielsen, Søren Jensby; Frydenvang, Karla Andrea; Johansen, Tommy Nørskov; Nielsen, Birgitte; Sehested, Maxwell; Jensen, Peter Buhl; Ikaunieks, Martins; Zaichenko, Andrei; Loza, Einars; Kalvinsh, Ivars; Björkling, Fredrik.

In: Journal of Medicinal Chemistry, Vol. 53, No. 19, 14.10.2010, p. 7140-7145.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Christensen, MK, Erichsen, KD, Trojel-Hansen, C, Tjørnelund, J, Nielsen, SJ, Frydenvang, KA, Johansen, TN, Nielsen, B, Sehested, M, Jensen, PB, Ikaunieks, M, Zaichenko, A, Loza, E, Kalvinsh, I & Björkling, F 2010, 'Synthesis and antitumor effect in vitro and in vivo of substituted 1,3-dihydroindole-2-ones', Journal of Medicinal Chemistry, vol. 53, no. 19, pp. 7140-7145. https://doi.org/10.1021/jm100763j

APA

Christensen, M. K., Erichsen, K. D., Trojel-Hansen, C., Tjørnelund, J., Nielsen, S. J., Frydenvang, K. A., ... Björkling, F. (2010). Synthesis and antitumor effect in vitro and in vivo of substituted 1,3-dihydroindole-2-ones. Journal of Medicinal Chemistry, 53(19), 7140-7145. https://doi.org/10.1021/jm100763j

Vancouver

Christensen MK, Erichsen KD, Trojel-Hansen C, Tjørnelund J, Nielsen SJ, Frydenvang KA et al. Synthesis and antitumor effect in vitro and in vivo of substituted 1,3-dihydroindole-2-ones. Journal of Medicinal Chemistry. 2010 Oct 14;53(19):7140-7145. https://doi.org/10.1021/jm100763j

Author

Christensen, Mette Knak ; Erichsen, Kamille Dumong ; Trojel-Hansen, Christina ; Tjørnelund, Jette ; Nielsen, Søren Jensby ; Frydenvang, Karla Andrea ; Johansen, Tommy Nørskov ; Nielsen, Birgitte ; Sehested, Maxwell ; Jensen, Peter Buhl ; Ikaunieks, Martins ; Zaichenko, Andrei ; Loza, Einars ; Kalvinsh, Ivars ; Björkling, Fredrik. / Synthesis and antitumor effect in vitro and in vivo of substituted 1,3-dihydroindole-2-ones. In: Journal of Medicinal Chemistry. 2010 ; Vol. 53, No. 19. pp. 7140-7145.

Bibtex

@article{0cd0b15b324b41fcaaa8d2d86d72b36a,
title = "Synthesis and antitumor effect in vitro and in vivo of substituted 1,3-dihydroindole-2-ones",
abstract = "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.",
keywords = "Former Faculty of Pharmaceutical Sciences",
author = "Christensen, {Mette Knak} and Erichsen, {Kamille Dumong} and Christina Trojel-Hansen and Jette Tj{\o}rnelund and Nielsen, {S{\o}ren Jensby} and Frydenvang, {Karla Andrea} and Johansen, {Tommy N{\o}rskov} and Birgitte Nielsen and Maxwell Sehested and Jensen, {Peter Buhl} and Martins Ikaunieks and Andrei Zaichenko and Einars Loza and Ivars Kalvinsh and Fredrik Bj{\"o}rkling",
year = "2010",
month = "10",
day = "14",
doi = "10.1021/jm100763j",
language = "English",
volume = "53",
pages = "7140--7145",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "19",

}

RIS

TY - JOUR

T1 - Synthesis and antitumor effect in vitro and in vivo of substituted 1,3-dihydroindole-2-ones

AU - Christensen, Mette Knak

AU - Erichsen, Kamille Dumong

AU - Trojel-Hansen, Christina

AU - Tjørnelund, Jette

AU - Nielsen, Søren Jensby

AU - Frydenvang, Karla Andrea

AU - Johansen, Tommy Nørskov

AU - Nielsen, Birgitte

AU - Sehested, Maxwell

AU - Jensen, Peter Buhl

AU - Ikaunieks, Martins

AU - Zaichenko, Andrei

AU - Loza, Einars

AU - Kalvinsh, Ivars

AU - Björkling, Fredrik

PY - 2010/10/14

Y1 - 2010/10/14

N2 - 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.

AB - 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.

KW - Former Faculty of Pharmaceutical Sciences

U2 - 10.1021/jm100763j

DO - 10.1021/jm100763j

M3 - Journal article

VL - 53

SP - 7140

EP - 7145

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 19

ER -

ID: 32330717