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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Cell Line, Tumor
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Dose-Response Relationship, Drug
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Humans
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Imidazoles / chemical synthesis
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Imidazoles / chemistry
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Imidazoles / pharmacology*
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Indoles / chemical synthesis
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Indoles / chemistry
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Indoles / pharmacology*
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Inhibitory Concentration 50
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Mice
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Mice, Nude
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Neoplasms / drug therapy
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Neoplasms / pathology
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Pyrroles / chemical synthesis
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Pyrroles / chemistry
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Pyrroles / pharmacology*
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Tumor Stem Cell Assay
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Xenograft Model Antitumor Assays
Substances
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Antineoplastic Agents
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Imidazoles
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Indoles
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Pyrroles
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topsentin A