Antitumor activity and COMPARE analysis of bis-indole derivatives
| Autor: | Cecilia Prata, Alessandra Locatelli, Alberto Leoni, Cristiana Caliceti, Francesco Vieceli Dalla Sega, Silvia Burnelli, Aldo Andreani, Robert H. Shoemaker, Massimiliano Granaiola, Laura Landi, Rita Morigi, Lucilla Varoli, Mirella Rambaldi |
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| Přispěvatelé: | Andreani A., Burnelli S., Granaiola M., Leoni A., Locatelli A., Morigi R., Rambaldi M., Varoli L., Landi L., Prata C., Vieceli Dalla Sega F., Caliceti C., Shoemaker R.H |
| Rok vydání: | 2010 |
| Předmět: |
Indoles
Stereochemistry Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Biochemistry Chemical synthesis ANTITUMOR Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound In vivo Cell Line Tumor Neoplasms Drug Discovery Pyridine COMPARE Humans Moiety Molecular Biology Cell Proliferation chemistry.chemical_classification Indole test Molecular Structure Bicyclic molecule INDOLE Organic Chemistry chemistry Lactam NQO1 Molecular Medicine Drug Screening Assays Antitumor PIRIDINE Lactone |
| Zdroj: | Bioorganic & Medicinal Chemistry. 18:3004-3011 |
| ISSN: | 0968-0896 |
| Popis: | This paper reports the synthesis of new derivatives (formed by two indole systems separated by a central moiety) analogous of potent antitumor agents previously described. The activity of the bis-indoles bearing a pyridine core confirms the good result described in the previous paper and compound 4c was chosen for the first in vivo experiment (Hollow Fiber Assay). COMPARE analysis and structure–activity relationships were also considered. Contrary to data reported by other Authors, no correlations were found between antitumor activity and NQO1 induction. |
| Databáze: | OpenAIRE |
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