olivacine/lukemia

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Synthesis and cytotoxic activity of hydroxylated derivatives of olivacine in relation with their biotransformation.

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Ingia / Ingia

The chemical synthesis of 9-hydroxyolivacine and 7-hydroxyolivacine based on a biomimetic approach is described. These two hydroxylated derivatives have been found as main in vitro metabolites of olivacine after incubation with rat hepatic microsomes. The pretreatment of animals with benzo[a]pyrene

Comparison of the pharmacological profile of an olivacine derivative and a potential prodrug.

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Ingia / Ingia

BACKGROUND The new olivacine derivative S 16020-2 (NSC-659687) has entered clinical trials on the basis of a marked antitumor activity in experimental models. Amongst the analogues which were synthesized to improve both therapeutic index and antitumor activity, the most active ones were those

Synthesis and biological evaluation of 6-(9-hydroxy-5-methyl (and 5,6-dimethyl)-6H-pyrido[4,3-b]carbazol-1-yl)picolinic amides as new olivacine derivatives.

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Ingia / Ingia

Starting from 2-(6-methoxy-1-methylcarbazol-2-yl)ethylamine and diethyl-2,6-pyridine dicarboxylate, the title compounds were obtained through five or six steps. The new compounds retained significant cytotoxicity towards various tumor cell lines, but in vivo studies on murine P388 leukemia, B16

In vivo antitumor activity of S 16020-2, a new olivacine derivative.

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Ingia / Ingia

The antitumor activity of S 16020-2, a new olivacine derivative, was investigated in vivo and compared with that of Adriamycin and elliptinium acetate in a panel of murine (P388 leukemia, M5076 sarcoma, Lewis lung carcinoma, and B16 melanoma) and human (NCI-H460 non-small-cell lung and MCF7 breast

In vitro and in vivo pharmacological characterizations of the antitumor properties of two new olivacine derivatives, S16020-2 and S30972-1.

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Ingia / Ingia

S16020-2, a new olivacine derivative and a topoisomerase II inhibitor, has recently entered clinical trials. New analogues and derivatives have been synthesized from the S16020-2 compound. Preliminary data indicate that S30972-1, one of these S16020-2 derivatives, may exhibit a comparatively higher

Synthesis and evaluation of 9-hydroxy-5-methyl-(and 5,6-dimethyl)-6H-pyrido[4,3-b]carbazole-1-N- [(dialkylamino)alkyl]carboxamides, a new promising series of antitumor olivacine derivatives.

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Ingia / Ingia

Starting from 2-(2-aminoethyl)-6-methoxy-1-methylcarbazole, ethyl 9-methoxy-5-methyl-6H-pyrido[4,3-b]carbazole-1-carboxylate was obtained through a three-step sequence. This compound and its 6-methyl derivative react with (dialkylamino)alkylamines to provide various

Synthesis and structure-activity relationship analysis of new olivacine derivatives.

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Ingia / Ingia

The number of 3'- and 4'-substituted 1-phenyl-6H-pyrido[4,3-b]carbazole derivatives have been synthesized and tested biologically. Eleven of the newly obtained compounds were subjected to the preliminary cytostatic screening for their activity against L1210 (murine leukemia), A498 (human kidney

DNA intercalating compounds as potential antitumor agents. 1. Preparation and properties of 7H-pyridocarbazoles.

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Ingia / Ingia

The DNA intercalating compounds derived from 6H-pyridocarbazole (ellipticines, olivacines) elicit high antitumor properties. In order to get information about the mechanism of action of these agents it is necessary to study structurally related analogues. For this purpose, various derivatives of the

Enhanced sensitivity to 1-beta-D-arabinofuranosylcytosine and topoisomerase II inhibitors in tumor cell lines harboring activated ras oncogenes.

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Ingia / Ingia

We used human tumor cell lines from the National Cancer Institute's In Vitro Antineoplastic Drug Screen to assess whether sensitivity to any of the approximately 45,000 compounds tested previously correlated with the presence of a ras oncogene. Among these cell lines, the mutations in Ki-ras2

New pyridocarbazole derivatives. Synthesis and their in vitro anticancer activity.

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Ingia / Ingia

In this paper, we describe our results of the synthesis and biological testing of analogues of the natural alkaloids olivacine and ellipticine. We have synthesized fourteen new 1-substituted pyrido[4,3-b]carbazole derivatives. All of them were tested in vitro for their anticancer activity on three

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