BLEDTA: tumor localization by a bleomycin analog containing a metal-chelating group
| Autor: | Leslie H. DeRiemer, Claude F. Meares, Carol I. Diamanti, David A. Goodwin |
|---|---|
| Rok vydání: | 1979 |
| Předmět: |
Adult
Male Bleomycin Mice chemistry.chemical_compound In vivo Neoplasms Drug Discovery medicine Animals Humans Distribution (pharmacology) Tissue Distribution Chelation Cobalt Radioisotopes Radionuclide Imaging Bifunctional Edetic Acid Chelating Agents Mice Inbred BALB C Cancer Neoplasms Experimental medicine.disease Molecular biology Squamous carcinoma chemistry Head and Neck Neoplasms Carcinoma Squamous Cell Molecular Medicine Derivative (chemistry) |
| Zdroj: | Journal of Medicinal Chemistry. 22:1019-1023 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00195a001 |
| Popis: | Two different Co(III) complexes of the antitumor antibiotic bleomycin have been prepared, and their in vivo distribution in mice has been investigated. The more thermodynamically stable of the Co(III)-bleomycin complexes has been modified by reaction with the bifunctional chelating agent 1-(p-bromoacetamidophenyl)ethylenedinitrilotetraacetic acid, to give a bleomycin derivative (BLEDTA) containing a powerful metal-chelating group. BLEDTA was radiolabeled with 111In(III) and its in vivo distribution in mice was examined. The potential of 111In-labeled BLEDTA as a tumor-visualizing agent was also investigated in humans with biopsy-proven cancers, predominantly (70%) squamous carcinoma of the head and neck. All of the 29 patients studied had at least one clinically proven site of the disease visualized with 111In-BLEDTA. These clinical results are significantly better than results we obtained in a comparable group of patients using directly labeled 111In-bleomycin and are similar to those reported by Nouel for 57Co-bleomycin [GANN Monogr. Cancer Res., 19, 301 (1976)]. |
| Databáze: | OpenAIRE |
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