Abstract |
A series of substituted ethyl 1-[(tert-butoxycarbonyl)amino]-2-methyl-5- (1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)carbonyl]-1H- pyrrole-3-carboxylates were prepared in excellent yields (82-98%) by one-pot reactions between β-dicarbonyl compounds 12a-e and 1,2-diaza-1,3-diene (DD) 13. Derivatives 10a,c-e, deazaanalogues of the bis- indole alkaloid topsentin, screened by the National Cancer Institute (Bethesda, MD, USA) in the in vitro one dose primary anticancer assay against a panel of about 60 human tumor cell lines, showed no significant activity, with the exception of compound 9e, which showed moderate activity against the HOP-92 cell line of the non small cell lung cancer sub-panel and the SNB-75 cell line of the CNS sub-panel.
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Authors | Anna Carbone, Virginia Spanò, Barbara Parrino, Cristina Ciancimino, Orazio A Attanasi, Gianfranco Favi |
Journal | Molecules (Basel, Switzerland)
(Molecules)
Vol. 18
Issue 3
Pg. 2518-27
(Feb 26 2013)
ISSN: 1420-3049 [Electronic] Switzerland |
PMID | 23442928
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Alkaloids
- Antineoplastic Agents
- Imidazoles
- Indoles
- topsentin
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Topics |
- Alkaloids
(chemistry, pharmacology)
- Antineoplastic Agents
(chemistry, pharmacology)
- Cell Line, Tumor
- Drug Screening Assays, Antitumor
- Humans
- Imidazoles
(chemistry, pharmacology)
- Indoles
(chemistry, pharmacology)
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