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2. 2,3-Bis(2-pyridyl)-5,8-quinoxalinediones with Metal Chelating Properties: Synthesis and Biological Evaluation

Author

Giorgi-Renault, Sylviane, Gebel-Servolles, Patricia, Helissey, Philippe, Renault, Jean, Bernier, Jean-Luc, Henichart, Jean-Pierre, and Cros, Suzanne

Abstract

The synthesis of 2,3-bis(2-pyridyl)-5,8-quinoxalinediones has been carried out in order to provide new antitumor drugs related to streptonigrin. Some derivatives have been found to possess significant cytotoxic properties and their mechanism of action has been studied. They were found to induce single-strand cleavage of covalently closed circular DNA (ccc-DNA). This biological activity requires an apparent in situ reduction (NADH activation) of the quinone to a hydroquinone or semiquinone radical, is facilitated by the presence of Cu(II), and involves activation of molecular oxygen to highly reactive radical species. Thus, although less active than the parent drugs, these molecules provide an attractive rationale for the observed cytotoxic and antitumor potency, as well as the cell-free single strand DNA cleavage efficacy of that family of drugs.

Published
1989
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5. Heterocyclic quinones. 17. A new in vivo active antineoplastic drug: 6,7-bis(1-aziridinyl)-4-[[3-(N,N-dimethylamino)propyl]amino]-5,8- quinazolinedione.

Author

Giorgi-Renault S, Renault J, Gebel-Servolles P, Baron M, Paoletti C, Cros S, Bissery MC, Lavelle F, and Atassi G

Subjects
Animals, Aziridines chemistry, Aziridines pharmacology, Aziridines therapeutic use, Breast Neoplasms, Cell Division drug effects, Cell Line, Drug Screening Assays, Antitumor, Female, Humans, Leukemia L1210, Leukemia, Experimental drug therapy, Melanoma, Experimental drug therapy, Mice, Mice, Inbred C57BL, Mice, Inbred DBA, Molecular Structure, Quinazolines chemistry, Quinazolines pharmacology, Quinazolines therapeutic use, Sarcoma, Experimental drug therapy, Structure-Activity Relationship, Antineoplastic Agents chemical synthesis, Aziridines chemical synthesis, Neoplasms, Experimental drug therapy, Quinazolines chemical synthesis
Abstract

A series of heterocyclic quinones, 6-substituted and 6,7-disubstituted 4-(alkylamino)-5,8-quinazolinediones, have been synthesized in order to evaluate their in vitro cytotoxicity on L1210 leukemia cells. Among 14 derivatives that have been prepared and studied for the structure-activity relationship, the most potent cytotoxic compound on L1210 leukemia cells was the 6,7-bis(1-aziridinyl)-4-[[3-(N,N-dimethylamino)propyl]amino]-5,8- quinazolinedione (24). This compound has been tested with the use of a cell-image processor on MCF-7 human mammary and HBL human melanoma cell lines. The results show that compound 24 influences cell proliferation and blocks both cells lines in the S phase. In vivo antineoplastic activity of compound 24 has been demonstrated on a broad spectrum of murine experimental models, but it was found highly toxic and produced long-delayed deaths.

Published
1991
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6. Heterocyclic quinones. XIII. Dimerization in the series of 5,8-quinazolinediones: synthesis and antitumor effects of bis(4-amino-5,8-quinazolinediones).

Author

Giorgi-Renault S, Renault J, Baron M, Gebel-Servolles P, Delic J, Cros S, and Paoletti C

Subjects
Animals, Cell Survival drug effects, Chemical Phenomena, Chemistry, Leukemia P388 drug therapy, Leukemia P388 pathology, Mice, Quinazolines pharmacology, Antineoplastic Agents chemical synthesis, Quinazolines chemical synthesis
Published
1988
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