Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin

Paola Barraja, Barbara Parrino, Virginia Spano', Patrizia Diana, Anna Carbone, Girolamo Cirrincione, Virginia Spanò, Heinz-Herbert Fiebig, Barbara Parrino, Anna Carbone, Paola Barraja, Girolamo Cirrincione, Patrizia Diana, Armin Maier, Gerhard Kelter

Risultato della ricerca: Article

54 Citazioni (Scopus)

Abstract

2,5-bis(3′-Indolyl)pyrroles, analogues of the marine alkaloid nortopsentin, were conveniently prepared through a three step procedure in good overall yields. Derivatives 1a and 1b exhibited concentration-dependent antitumor activity towards a panel of 42 human tumor cell lines with mean IC50 values of 1.54 μM and 0.67 μM, respectively. Investigating human tumor xenografts in an ex-vivo clonogenic assay revealed selective antitumor activity, whereas sensitive tumor models were scattered among various tumor histotypes.
Lingua originaleEnglish
pagine (da-a)643-654
Numero di pagine12
RivistaMarine Drugs
Volume11
Stato di pubblicazionePublished - 2013

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Pyrroles
Alkaloids
Neoplasms
Tumor Cell Line
Heterografts
Inhibitory Concentration 50

All Science Journal Classification (ASJC) codes

  • Drug Discovery

Cita questo

Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin. / Barraja, Paola; Parrino, Barbara; Spano', Virginia; Diana, Patrizia; Carbone, Anna; Cirrincione, Girolamo; Spanò, Virginia; Fiebig, Heinz-Herbert; Parrino, Barbara; Carbone, Anna; Barraja, Paola; Cirrincione, Girolamo; Diana, Patrizia; Maier, Armin; Kelter, Gerhard.

In: Marine Drugs, Vol. 11, 2013, pag. 643-654.

Risultato della ricerca: Article

Barraja, P, Parrino, B, Spano', V, Diana, P, Carbone, A, Cirrincione, G, Spanò, V, Fiebig, H-H, Parrino, B, Carbone, A, Barraja, P, Cirrincione, G, Diana, P, Maier, A & Kelter, G 2013, 'Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin', Marine Drugs, vol. 11, pagg. 643-654.
Barraja, Paola ; Parrino, Barbara ; Spano', Virginia ; Diana, Patrizia ; Carbone, Anna ; Cirrincione, Girolamo ; Spanò, Virginia ; Fiebig, Heinz-Herbert ; Parrino, Barbara ; Carbone, Anna ; Barraja, Paola ; Cirrincione, Girolamo ; Diana, Patrizia ; Maier, Armin ; Kelter, Gerhard. / Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin. In: Marine Drugs. 2013 ; Vol. 11. pagg. 643-654.
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abstract = "2,5-bis(3′-Indolyl)pyrroles, analogues of the marine alkaloid nortopsentin, were conveniently prepared through a three step procedure in good overall yields. Derivatives 1a and 1b exhibited concentration-dependent antitumor activity towards a panel of 42 human tumor cell lines with mean IC50 values of 1.54 μM and 0.67 μM, respectively. Investigating human tumor xenografts in an ex-vivo clonogenic assay revealed selective antitumor activity, whereas sensitive tumor models were scattered among various tumor histotypes.",
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author = "Paola Barraja and Barbara Parrino and Virginia Spano' and Patrizia Diana and Anna Carbone and Girolamo Cirrincione and Virginia Span{\`o} and Heinz-Herbert Fiebig and Barbara Parrino and Anna Carbone and Paola Barraja and Girolamo Cirrincione and Patrizia Diana and Armin Maier and Gerhard Kelter",
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T1 - Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin

AU - Barraja, Paola

AU - Parrino, Barbara

AU - Spano', Virginia

AU - Diana, Patrizia

AU - Carbone, Anna

AU - Cirrincione, Girolamo

AU - Spanò, Virginia

AU - Fiebig, Heinz-Herbert

AU - Parrino, Barbara

AU - Carbone, Anna

AU - Barraja, Paola

AU - Cirrincione, Girolamo

AU - Diana, Patrizia

AU - Maier, Armin

AU - Kelter, Gerhard

PY - 2013

Y1 - 2013

N2 - 2,5-bis(3′-Indolyl)pyrroles, analogues of the marine alkaloid nortopsentin, were conveniently prepared through a three step procedure in good overall yields. Derivatives 1a and 1b exhibited concentration-dependent antitumor activity towards a panel of 42 human tumor cell lines with mean IC50 values of 1.54 μM and 0.67 μM, respectively. Investigating human tumor xenografts in an ex-vivo clonogenic assay revealed selective antitumor activity, whereas sensitive tumor models were scattered among various tumor histotypes.

AB - 2,5-bis(3′-Indolyl)pyrroles, analogues of the marine alkaloid nortopsentin, were conveniently prepared through a three step procedure in good overall yields. Derivatives 1a and 1b exhibited concentration-dependent antitumor activity towards a panel of 42 human tumor cell lines with mean IC50 values of 1.54 μM and 0.67 μM, respectively. Investigating human tumor xenografts in an ex-vivo clonogenic assay revealed selective antitumor activity, whereas sensitive tumor models were scattered among various tumor histotypes.

KW - antitumor

KW - bis-indolyl-pyrroles

KW - ex-vivo xenografts

KW - marine alkaloids

KW - nortopsentin analogues

UR - http://hdl.handle.net/10447/72063

M3 - Article

VL - 11

SP - 643

EP - 654

JO - Marine Drugs

JF - Marine Drugs

SN - 1660-3397

ER -