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Your search keyword '"Pindur, A."' showing total 7 results
Start Over Author "Pindur, A." Journal european journal of medicinal chemistry
7 results on '"Pindur, A."'

5. Photochemical electrocyclisation of 3-vinylindoles to pyrido[2,3-a]-, pyrido[4,3-a]- and thieno[2,3-a]-carbazoles: Design, synthesis, DNA binding and antitumor cell cytotoxicity

Author

Marie-Hélène David-Cordonnier, Thomas Lemster, Gaëlle Lenglet, Ulf Pindur, Christelle Dassi, and Sabine Depauw

Subjects
Indoles, Cell Survival, Stereochemistry, Carbazoles, Fluorescence spectrometry, Antineoplastic Agents, Stereoisomerism, Context (language use), Nucleic Acid Denaturation, Chemical synthesis, Fluorescence, Structure-Activity Relationship, Cell Line, Tumor, Drug Discovery, Animals, Humans, Topoisomerase II Inhibitors, Transition Temperature, Structure–activity relationship, Binding site, Cell Proliferation, Pharmacology, Binding Sites, biology, Chemistry, Circular Dichroism, Topoisomerase, Cell Cycle, Organic Chemistry, DNA, General Medicine, Photochemical Processes, DNA Minor Groove Binding, Cyclization, Drug Design, biology.protein, Cattle, Spectrophotometry, Ultraviolet, Topoisomerase I Inhibitors
Abstract

In the context of the design and synthesis of DNA ligands, some new hetarene annelated carbazoles were synthesized. As lead structure the intercalating tetracyclic systems pyrido[2,3-a]- and pyrido[4,3-a]-carbazoles and in one case a thieno[2,3-a]-carbazole were taken into account. A dialkyl amino amidic chain was introduced to the planar chromophoric system with the intent to generate minor groove binding properties. The cytotoxicity of some compounds was examined by the NCI antitumor screening. Furthermore, biophysical as well as biochemical studies were performed in order to get some information about the DNA-binding properties and inhibition of DNA related functional enzymes of this new series of molecules.

Published
2009

6. New propylamine oligopyrrole carboxamides linked to a heterocyclic or anthraquinone system: synthesis, DNA binding, topoisomerase I inhibition and cytotoxicity

Author

Christian Hotzel, Annalisa Marotto, and Ulf Pindur

Subjects
Tertiary amine, Stereochemistry, Oligonucleotides, Anthraquinones, Antineoplastic Agents, Propylamine, Nucleic Acid Denaturation, Anthraquinone, Chemical synthesis, chemistry.chemical_compound, Drug Discovery, Tumor Cells, Cultured, medicine, Animals, Humans, Cytotoxicity, Pharmacology, Propylamines, biology, Topoisomerase, Distamycins, Organic Chemistry, Netropsin, DNA, General Medicine, Ligand (biochemistry), Intercalating Agents, Mechanism of action, chemistry, biology.protein, Nucleic Acid Conformation, Cattle, Topoisomerase I Inhibitors, medicine.symptom
Abstract

Continuing our studies on combilexines, compounds consisting of a DNA intercalator linked to a minor groove ligand, new results are presented. The synthesis of a series of new propylamine oligopyrrole carboxamides closely related to netropsin and distamycin A, linked to a heterocyclic or anthraquinone system is reported. The cytotoxic activity in vitro, the DNA binding characteristics and the inhibition of the topoisomerase I of the compounds were studied in order to explain the biological mechanism of action of these new potential combilexines. Some of the synthesised compounds showed cytotoxic activity against human tumour cell lines, as well as DNA binding and topoisomerase I inhibiting properties.

Published
2003

7. Design, synthesis and biological evaluation of new oligopyrrole carboxamides linked with tricyclic DNA-intercalators as potential DNA ligands or topoisomerase inhibitors

Author

Thomas Lemster, Brigitte Baldeyrou, Amélie Lansiaux, Marie-Paule Hildebrand, Ulf Pindur, Christoph Keuser, Kerstin Benzschawel, and Marie-Hélène David-Cordonnier

Subjects
Stereochemistry, medicine.drug_class, Topoisomerase Inhibitors, DNA Footprinting, Context (language use), Antineoplastic Agents, Ligands, chemistry.chemical_compound, Structure-Activity Relationship, Cell Line, Tumor, Drug Discovery, medicine, Structure–activity relationship, Humans, Pyrroles, Pharmacology, biology, Molecular Structure, Chemistry, Topoisomerase, Organic Chemistry, Distamycins, Netropsin, General Medicine, DNA, DNA Minor Groove Binding, Intercalating Agents, Acridone, Drug Design, Acridine, biology.protein, Topoisomerase inhibitor
Abstract

In the context of the design and synthesis of minor groove binding and intercalating DNA ligands some new oligopyrrole carboxamides were synthesized. These hybrid molecules (combilexins) possess a variable and conformatively flexible spacer at the N-terminal end. As intercalating tricyclic systems acridone, acridine, anthraquinones and in a special case iminostilbene terminate the N-terminal end of the pyrrole chain. The cytotoxicity was examined by the NCI antitumor screening, furthermore, biophysical as well as biochemical studies were performed in order to get some information about the DNA binding properties and topoisomerase inhibition effect of this new series of molecules.

Published
2006

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