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C Malvy

Publications and source records attributed to C Malvy.

65 records · Page 4Linked to original sources
PubMed1986

Efficient breakage of DNA apurinic sites by the indoleamine related 9-amino-ellipticine.

The aromatic amine, 9-NH2-ellipticine, is a synthetic DNA intercalating derivative of the antitumor agent ellipticine, which breaks circular DNA containing apurinic sites. This breakage is inhibited when the apurinic (AP) sites are reduced. The concentration of 9-NH2-ellipticine required to get a significant effect (0.1 microM) is the lowest known among chemicals which induce the same breakage reaction. Comparison with the action of structurally related amines shows that the amino-indole structure is specific for AP sites. The ability of ellipticine derivatives to induce breakage in DNA containing apurinic sites is related to the nucleophile substituent in position 9. Two ellipticine derivatives with known antitumor activity, BD 40 and 9-OH-ellipticine, were able to break purified DNA at apurinic sites.

Alkaloids↗
PubMed1981

Ellipticine, 9-hydroxyellipticine, and 9-hydroxyellipiticinum: some biochemical properties of possible pharmacologic significance.

Ellipticine, 5,11-dimethyl-(6H)-pyrido-(4,3,b)-carbazole (NSC 71795) is a potent cytotoxic and antitumor agent. Several of its derivatives share these properties and nine hydroxylated compounds are even more potent. 2-Methyl-9-hydorxyellipticinium (NSC 264-137) has thus recently been shown to display some therapeutic effectiveness in human breast cancers. The biochemical mechanism of this action is discussed in this paper. DNA has been implied as the target of ellipticine and some derivatives; however, these drugs do not break DNA in cultured L1210 cells. Moreover, several other biochemical constituents are able to bind these compounds in vitro as efficiently as DNA. In this paper the interactions between ellipticine and some of those derivatives and (a) ascitic phospholipids monolayers and (b) cytochrome P450 microsomal proteins are studied and discussed. Finally, the hypothesis that the nonhydroxylated ellipticine derivatives might be better cytotoxic agents because they can be oxidized and generate free radical species through a monovalent electron transfer process is presented. This hypothesis is supported by experiments carried out on the oxidation of 9-hydroxyellipticine and 2-methyl-9-hydroxyellipticine by peroxidases.

Alkaloids↗
PubMed1980

[9-Nitro- and 9-amino-ellipticines and derivatives: synthesis and pharmacologic properties].

Preparation of 9-nitroellipticine starting from 1,4-dimethyl-6-nitrocarbazole and its reduction according to the Béchamp method followed by acetylation. The salts of 9-nitro-2-methyl- and 9-amino-2-methyl ellipticinium were tested for cytotoxic activity on different tumor strains for mutagenicity, for affinity for DNA and cytochrome P450 and for toxicity in the mouse. The results obtained were compared with those found under the same conditions with 9-hydroxyellipticine and its corresponding ellipticinium salt.

Alkaloids↗
PubMedDate not supplied

Covalent coupling of a PIM-1 oncogene targeted PNA with an antennapedia derived peptide.

Peptide nucleic acids (PNA) are promising antisense molecule for blocking gene expression in cell culture or in vivo. Nevertheless because they are poor efficient to pass the cellular membrane, it is necessary to use a vectorisation agent to observe an inhibitory effect. We describe the coupling of the rhodamine labeled 17-mer antisense PNA to a fusogenic peptide from antenapedia via S-S linkage, the studies of the penetration of this complex into fibroblast cells and its inhibitory effect on pim1 targeted protononcogene.

3T3 Cells↗