3,5-BIS(3’-INDOLYL)PYRAZOLES, ANALOGUES OF MARINE ALKALOID NORTOPSENTIN: SYNTHESIS AND ANTITUMOR PROPERTIES

Risultato della ricerca: Article

67 Citazioni (Scopus)

Abstract

A series of bis-indolylpyrazoles were obtained by cyclization of diketones using hydrazine monohydrate or methylhydrazine in refluxing acetic acid/THF. Three of the derivs. were selected, by the National Cancer Institute (NCI, Bethesda, USA), to be evaluated against the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity in the micromolar range. In particular, I, the most active compd. was effective against all the tested cell lines with a GI50 mean value of 3.23 μM; TGI and LC50 values were 14.5 and 58.9 μM having pos. response on 91% and 41% of the tested cell lines, resp.
Lingua originaleEnglish
pagine (da-a)6134-6137
RivistaBIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume17
Stato di pubblicazionePublished - 2007

Fingerprint

Pyrazoles
Alkaloids
Cells
hydrazine
Monomethylhydrazine
Cyclization
Acetic Acid
Tumors

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Organic Chemistry
  • Clinical Biochemistry
  • Drug Discovery
  • Pharmaceutical Science
  • Molecular Biology
  • Molecular Medicine

Cita questo

@article{8b4a99a45c9b4947890c4c25d7dc3120,
title = "3,5-BIS(3’-INDOLYL)PYRAZOLES, ANALOGUES OF MARINE ALKALOID NORTOPSENTIN: SYNTHESIS AND ANTITUMOR PROPERTIES",
abstract = "A series of bis-indolylpyrazoles were obtained by cyclization of diketones using hydrazine monohydrate or methylhydrazine in refluxing acetic acid/THF. Three of the derivs. were selected, by the National Cancer Institute (NCI, Bethesda, USA), to be evaluated against the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity in the micromolar range. In particular, I, the most active compd. was effective against all the tested cell lines with a GI50 mean value of 3.23 μM; TGI and LC50 values were 14.5 and 58.9 μM having pos. response on 91{\%} and 41{\%} of the tested cell lines, resp.",
author = "Girolamo Cirrincione and Paola Barraja and Patrizia Diana and Annamaria Martorana and Anna Carbone and Lisa Dallavia and Ornella Gia",
year = "2007",
language = "English",
volume = "17",
pages = "6134--6137",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Ltd",

}

TY - JOUR

T1 - 3,5-BIS(3’-INDOLYL)PYRAZOLES, ANALOGUES OF MARINE ALKALOID NORTOPSENTIN: SYNTHESIS AND ANTITUMOR PROPERTIES

AU - Cirrincione, Girolamo

AU - Barraja, Paola

AU - Diana, Patrizia

AU - Martorana, Annamaria

AU - Carbone, Anna

AU - Dallavia, Lisa

AU - Gia, Ornella

PY - 2007

Y1 - 2007

N2 - A series of bis-indolylpyrazoles were obtained by cyclization of diketones using hydrazine monohydrate or methylhydrazine in refluxing acetic acid/THF. Three of the derivs. were selected, by the National Cancer Institute (NCI, Bethesda, USA), to be evaluated against the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity in the micromolar range. In particular, I, the most active compd. was effective against all the tested cell lines with a GI50 mean value of 3.23 μM; TGI and LC50 values were 14.5 and 58.9 μM having pos. response on 91% and 41% of the tested cell lines, resp.

AB - A series of bis-indolylpyrazoles were obtained by cyclization of diketones using hydrazine monohydrate or methylhydrazine in refluxing acetic acid/THF. Three of the derivs. were selected, by the National Cancer Institute (NCI, Bethesda, USA), to be evaluated against the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity in the micromolar range. In particular, I, the most active compd. was effective against all the tested cell lines with a GI50 mean value of 3.23 μM; TGI and LC50 values were 14.5 and 58.9 μM having pos. response on 91% and 41% of the tested cell lines, resp.

UR - http://hdl.handle.net/10447/17356

M3 - Article

VL - 17

SP - 6134

EP - 6137

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

ER -