Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin
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...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2013-03-01
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| Series: | Marine Drugs |
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| Online Access: | http://www.mdpi.com/1660-3397/11/3/643 |
| _version_ | 1798005109488091136 |
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| author | Gerhard Kelter Armin Maier Patrizia Diana Girolamo Cirrincione Virginia Spanò Paola Barraja Barbara Parrino Anna Carbone Heinz-Herbert Fiebig |
| author_facet | Gerhard Kelter Armin Maier Patrizia Diana Girolamo Cirrincione Virginia Spanò Paola Barraja Barbara Parrino Anna Carbone Heinz-Herbert Fiebig |
| author_sort | Gerhard Kelter |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-04-11T12:35:03Z |
| format | Article |
| id | doaj.art-f3dd1038506f4ec08099288a9432a97a |
| institution | Directory Open Access Journal |
| issn | 1660-3397 |
| language | English |
| last_indexed | 2024-04-11T12:35:03Z |
| publishDate | 2013-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Marine Drugs |
| spelling | doaj.art-f3dd1038506f4ec08099288a9432a97a2022-12-22T04:23:40ZengMDPI AGMarine Drugs1660-33972013-03-0111364365410.3390/md11030643Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid NortopsentinGerhard KelterArmin MaierPatrizia DianaGirolamo CirrincioneVirginia SpanòPaola BarrajaBarbara ParrinoAnna CarboneHeinz-Herbert Fiebig2,5-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.http://www.mdpi.com/1660-3397/11/3/643bis-indolyl-pyrrolesnortopsentin analoguesmarine alkaloidsantitumorex-vivo xenografts |
| spellingShingle | Gerhard Kelter Armin Maier Patrizia Diana Girolamo Cirrincione Virginia Spanò Paola Barraja Barbara Parrino Anna Carbone Heinz-Herbert Fiebig Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin Marine Drugs bis-indolyl-pyrroles nortopsentin analogues marine alkaloids antitumor ex-vivo xenografts |
| title | Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin |
| title_full | Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin |
| title_fullStr | Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin |
| title_full_unstemmed | Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin |
| title_short | Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin |
| title_sort | synthesis and antiproliferative activity of 2 5 bis 3 indolyl pyrroles analogues of the marine alkaloid nortopsentin |
| topic | bis-indolyl-pyrroles nortopsentin analogues marine alkaloids antitumor ex-vivo xenografts |
| url | http://www.mdpi.com/1660-3397/11/3/643 |
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