Ellipticine derivatives with an affinity to the estrogen receptor. An approach to develop intercalating drugs with a specific effect on the hormone-dependent breast cancer
| Autor: | Bernard P. Roques, Jean Bernard Le Pecq, Alain Delbarre, Henri Rochefort, Jean Louis Borgna, Alain Jacquemin-Sablon, Robert Oberlin |
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| Rok vydání: | 1985 |
| Předmět: |
Neoplasms
Hormone-Dependent medicine.medical_treatment Estrogen receptor Breast Neoplasms Estrone In Vitro Techniques Cell Line Steroid chemistry.chemical_compound Alkaloids Breast cancer Drug Discovery medicine Animals Humans Ellipticines Leukemia L1210 Cytotoxicity Chemistry Alkaloid DNA medicine.disease Intercalating Agents DNA Intercalation Receptors Estrogen Biochemistry Cancer research Molecular Medicine Cattle Female |
| Zdroj: | Journal of Medicinal Chemistry. 28:752-761 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00383a011 |
| Popis: | In order to obtain breast tumor directed agents, we have prepared mixed compounds using estradiol or (E)-clomiphene as specific vectors of the breast tissue and a DNA intercalator from the ellipticine series as the cytotoxic agent. Among the newly synthesized ellipticine derivatives, only the 2-[3-aza-5-(3,17 beta-dihydroxy-1,3,5-estratrien-17 alpha-yl)-4-oxopentamethylene]ellipticinium bromide shows the desired properties, DNA intercalation and affinity for estrogen receptor. Competition experiments with estradiol on the hormone-dependent human MCF-7 breast cancer cell line demonstrate that a transport by the estrogen receptor system is not involved in the antitumor activity of derivative 24. |
| Databáze: | OpenAIRE |
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