Boron-Containing Polyamines as DNA Targeting Agents for Neutron Capture Therapy of Brain Tumors: Synthesis and Biological Evaluation
| Autor: | Iwona M. Wyzlic, Jianping Cai, Joya R. Hariharan, Krista Radcliffe, Dianne M. Adams, Rolf F. Barth, Albert H. Soloway |
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| Rok vydání: | 1997 |
| Předmět: |
Boron Compounds
Spermidine Spermine Antineoplastic Agents Boron Neutron Capture Therapy Structure-Activity Relationship chemistry.chemical_compound Pregnancy Glioma Drug Discovery Tumor Cells Cultured medicine Animals Cytotoxicity Brain Neoplasms DNA medicine.disease Rats Inbred F344 In vitro Rats chemistry Biochemistry Molecular Medicine Female Ethidium bromide Polyamine |
| Zdroj: | Journal of Medicinal Chemistry. 40:3887-3896 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | Three series of new boron-containing spermidine/spermine (SPD/SPM) analogues have been synthesized: N1- and N5-(4-carboranylbutyl) SPD/SPM derivatives (SPD-1, SPD-5, SPM-1, SPM-5); N1,N10-diethyl-N5-(4-carboranylbutyl)spermidine (DESPD-5), N1,N14-diethyl-N5-(4-carboranylbutyl)spermine (DESPM-5); and N5,N10-bis(4-carboranylbutyl)spermine (SPM-5,10). In vitro studies using rat F98 glioma cells have shown that these polyamines retain the ability to displace ethidium bromide from calf thymus DNA and are rapidly taken up by F98 glioma cells. However, their cytotoxicities, especially those with terminal N-substituted (SPD-1, SPM-1) boron compounds, are greater than those of SPD/SPM. Nevertheless, the groundwork has been created for a new class of boron-containing compounds that maybe useful for boron neutron capture therapy of tumors. |
| Databáze: | OpenAIRE |
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