Search results for: Brigitte Baldeyrou

Items from 1 to 20 out of 33 results

article

Synthesis and biological activity of ferrocenyl indeno[1,2-c]isoquinolines as topoisomerase II inhibitors

Nathalie Wambang, Nadège Schifano-Faux, Alexandre Aillerie, Brigitte Baldeyrou, more

Bioorganic & Medicinal Chemistry > 2016 > 24 > 4 > 651-660

Three series of indeno[1,2-c]isoquinolines bearing a ferrocenyl entity were synthesized and evaluated for DNA interaction, topoisomerase I and II inhibition, and cytotoxicity against breast human cancer cell lines. In the first and second series, the ferrocenyl scaffold was inserted as a linker between the two nitrogen atoms. In the last series, it was introduced at the end of the carbon chain. The...

article

Synthesis of new biologically active isothiazolo[4,5-b]carbazole-type tetracyclic derivatives via an indole-2,3-quinodimethane approach

Raimundo F. Miambo, Marie Laronze-Cochard, Ata-Martin Lawson, Régis Guillot, more

Tetrahedron > 2014 > 70 > 44 > 8286-8302

A number of isothiazolo[4,5-b]carbazole derivatives were prepared via a Diels–Alder approach involving thermally induced indole-2,3-quinodimethane intermediates. Preliminary biological tests revealed a GSK-3β kinase inhibitor (29) and some free NH group containing compounds (17d, 19c, 29) displayed selective human carbonic anhydrase I inhibitory activities.

article

Low level of baseline circulating VEGF-A is associated with better outcome in patients with vascular sarcomas receiving sorafenib: an ancillary study from a phase II trial

Nicolas Penel, Isabelle Ray-Coquard, Christine Bal-Mahieu, Christine Chevreau, more

Targeted Oncology > 2014 > 9 > 3 > 273-277

We have carried out a stratified phase II study of sorafenib (So) in patients with advanced angiosarcoma (n = 32) and epithelioid hemangioendothelioma (n = 13). This report concerns the correlative analysis of the predictive values of circulating pro/anti-angiogenetic biomarkers. Using the ELISA method (R&D Systems), circulating biomarkers (VEGF-A, in picograms per milliliter), thrombospondin-1...

article

Synthesis, antiproliferative activity and tubulin targeting effect of acridinone and dioxophenothiazine derivatives

Valérie Verones, Nathalie Flouquet, Marie Lecoeur, Amelie Lemoine, more

European Journal of Medicinal Chemistry > 2013 > 59 > Complete > 39-47

The synthesis of new acridinone and dioxophenothiazine derivatives along with their tubulin polymerization inhibitory and antiproliferative activities is reported. The analysis of correlation for cytotoxic and antitubulin potential of tested compounds showed that 4-methoxyphenylethyl derivatives 18a and 19a were highly cytotoxic but were regarded to have no significant antitubulin activity. However,...

article

Synthesis of chromeno[3,4-b]indoles as Lamellarin D analogues : A novel DYRK1A inhibitor class

Cleopatra Neagoie, Emeline Vedrenne, Frédéric Buron, Jean-Yves Mérour, more

European Journal of Medicinal Chemistry > 2012 > 49 > Complete > 379-396

A library of substituted chromeno[3,4-b]indoles was developed as Lamellarin isosters. Synthesis was achieved from indoles after a four-step pathway sequence involving C-3 iodination, a Suzuki cross-coupling reaction, and a one pot deprotection/lactonisation step. Twenty final compounds were tested in order to determine their activity against topoisomerase I and kinases, the two major biological activities...

article

Synthesis, cytotoxicity and topoisomerase inhibition properties of multifarious aminoalkylated indeno[1,2-c]isoquinolin-5,11-diones

Gang Ahn, Nadège Schifano-Faux, Jean-François Goossens, Brigitte Baldeyrou, more

Bioorganic & Medicinal Chemistry Letters > 2011 > 21 > 8 > 2259-2263

A number of mono- or diaminoalkylated indeno[1,2-c]isoquinolin-5,11-diones analogs of 1 were synthesized and evaluated for their DNA binding affinities, topoisomerase inhibition properties and antiproliferative activities against human cancer cell lines (HL60). Impact of the side chain connected to the aromatic D ring and to the N6 lactam position on the biological profile will be discussed.

article

Toward new camptothecins. Part 7: Synthesis of thioluotonin and its 5-methoxycarbonyl derivative

Thomas Boisse, Laurent Gavara, Philippe Gautret, Brigitte Baldeyrou, more

Tetrahedron Letters > 2011 > 52 > 14 > 1592-1596

The synthesis of thiodeoxyvasicinone and thioluotonin derivatives is described. The results obtained indicate that in these series, oxygen to sulfur replacement leads to absence of strong interaction with topoisomerase I-DNA.

article

Design, Synthesis, and DNA-Binding of N -Alkyl(anilino)quinazoline Derivatives

Antonio Garofalo, Laurence Goossens, Brigitte Baldeyrou, Amélie Lemoine, more

Journal of Medicinal Chemistry > 2010 > 53 > 22 > 8089 - 8103

article

Indeno[1,2-c]isoquinolin-5,11-diones conjugated to amino acids: Synthesis, cytotoxicity, DNA interaction, and topoisomerase II inhibition properties

Gang Ahn, Amélie Lansiaux, Jean-François Goossens, Christian Bailly, more

Bioorganic & Medicinal Chemistry > 2010 > 18 > 22 > 8119-8133

Three series of indeno[1,2-c]isoquinolin-5,11-dione-amino acid conjugates were designed and synthesized. Amino acids were connected to the tetracycle through linkers with lengths of n=2 and 3 atoms using ester (series I), amide (series II), and secondary amine (series III) functions. DNA binding was evaluated by thermal denaturation and fluorescence measurements. Lysine and arginine substituted derivatives...

article

Synthesis and biological activities of new furo[3,4-b]carbazoles: Potential topoisomerase II inhibitors

Youssef Hajbi, Cléopatra Neagoie, Bérenger Biannic, Aurélie Chilloux, more

European Journal of Medicinal Chemistry > 2010 > 45 > 11 > 5428-5437

New 1,5-Dihydro-4-(substituted phenyl)-3H-furo[3,4-b]carbazol-3-ones were synthesised via a key step Diels–Alder reaction under microwave irradiation. 3-Formylindole was successfully used in a 6-step synthesis to obtain those complex heterocycles. The Diels–Alder reaction generating the carbazole ring was optimised under thermal conditions or microwave irradiation. After cleavage of functional groups,...

article

Montmorillonite K-10 catalyzed cyclization of N-ethoxycarbonyl-N′-arylguanidines: Access to pyrimido[4,5-c]carbazole and pyrimido[5,4-b]indole derivatives

Julien Debray, Walid Zeghida, Brigitte Baldeyrou, Christine Mahieu, more

Bioorganic & Medicinal Chemistry Letters > 2010 > 20 > 14 > 4244-4247

Two new heterocycles, pyrimido[4,5-c]carbazole and pyrimido[5,4-b]indole, were prepared in three steps from 3-aminocarbazole and 3-aminoindole, respectively. The key Friedel–Crafts intramolecular cyclization was realized under microwave irradiation using montmorillonite K-10 clay as a catalyst. The pyrimido[4,5-c]carbazole derivative shows significant micromolar IC ₅₀ against cancer cell lines...

article

Synthesis and antitumoral activity of novel thiazolobenzotriazole, thiazoloindolo[3,2-c]quinoline and quinolinoquinoline derivatives

Anne Beauchard, Alexis Jaunet, Laurence Murillo, Brigitte Baldeyrou, more

European Journal of Medicinal Chemistry > 2009 > 44 > 10 > 3858-3865

The biological evaluation of some novel thiazoloindolo[3,2-c]quinoline, 8-substituted-11H-indolo[3,2-c]quinolines is described. These compounds were obtained via Graebe–Ullmann thermal cyclization from appropriated N-arylated benzotriazoles. 7H-4,7-Diaza-benzo[de]anthracene, a reaction by-product structurally closed to the pyridoacridine skeleton was also identified. All thiazolobenzotriazole intermediates...

article

Synthesis, Cytotoxicity, DNA Interaction, and Topoisomerase II Inhibition Properties of Novel Indeno[2,1- c ]quinolin-7-one and Indeno[1,2- c ]isoquinolin-5,11-dione Derivatives

Adina Ryckebusch, Deborah Garcin, Amélie Lansiaux, Jean-François Goossens, more

Journal of Medicinal Chemistry > 2008 > 51 > 12 > 3617 - 3629

article

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

Marie-Hélène David-Cordonnier, Marie-Paule Hildebrand, Brigitte Baldeyrou, Amelie Lansiaux, more

European Journal of Medicinal Chemistry > 2007 > 42 > 6 > 752-771

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...

article

Amino- and glycoconjugates of pyrido[4,3,2-kl]acridine. Synthesis, antitumor activity, and DNA binding

Laurent Bouffier, Brigitte Baldeyrou, Marie-Paule Hildebrand, Amélie Lansiaux, more

Bioorganic & Medicinal Chemistry > 2006 > 14 > 22 > 7520-7530

A series of amino- and glycoconjugates of pyrido[4,3,2-kl]acridine and pyrido[4,3,2-kl]acridin-4-one have been prepared. The most active molecules, the amino conjugates 7 and 11, display a cytostatic activity against HT-29 cancer cells at micromolar concentration. This activity correlates well with a strong DNA binding. The molecules, amino or glycoconjugates, bind DNA by intercalation, the amino...

article

Synthesis of 2,6-diphenylpyrazine derivatives and their DNA binding and cytotoxic properties

Nathalie Dias, Ulrich Jacquemard, Brigitte Baldeyrou, Amélie Lansiaux, more

European Journal of Medicinal Chemistry > 2005 > 40 > 12 > 1206-1213

A series of 2,6-diphenylpyrazine derivatives was synthesized from 2,6-dichloropyrazine and 4-methoxyphenylboronic acid using palladium(0) as catalyst in a Suzuki methodology. After deprotection of the hydroxyl, alkylation reactions with different halides afforded compounds 5–8 bearing hydrophilic chains. DNA binding and cytotoxic properties were investigated. Compound 11 bearing imidazoline terminal...

article

Oxoazabenzo[ de ]anthracenes Conjugated to Amino Acids: Synthesis and Evaluation as DNA-Binding Antitumor Agents

Nathalie Dias, Jean-François Goossens, Brigitte Baldeyrou, Amélie Lansiaux, more

Bioconjugate Chemistry > 2005 > 16 > 4 > 949 - 958

article

Targeting DNA with Novel Diphenylcarbazoles ^†

Nathalie Dias, Ulrich Jacquemard, Brigitte Baldeyrou, Christelle Tardy, more

Biochemistry > 2004 > 43 > 48 > 15169 - 15178

article

Novel antitumor indenoindole derivatives targeting DNA and topoisomerase II

Christine Bal, Brigitte Baldeyrou, Florence Moz, Amélie Lansiaux, more

Biochemical Pharmacology > 2004 > 68 > 10 > 1911-1922

We have identified a novel series of indenoindole derivatives endowed with potent cytotoxic activities toward cancer cells. Five compounds containing a 8-[2-(dialkylamino)ethoxy]-2,3-dimethoxy-5H-10H-indeno[1,2-b]indol-10-one-O-propynyl-oxime core substituted with a phenyl, furanyl, or a methyl substituent on the propynyl side chain have been synthesized and their mechanism of action was investigated...

article

Synthesis and cytotoxic activity of benzo[c][1,7] and [1,8]phenanthrolines analogues of nitidine and fagaronine

Soizic Prado, Sylvie Michel, François Tillequin, Michel Koch, more

Bioorganic & Medicinal Chemistry > 2004 > 12 > 14 > 3943-3953

Fagaronine and nitidine are natural benzo[c] phenanthridinium alkaloids, which display antileukemic activity. Both act as topoisomerase I and topoisomerase II inhibitors. The objective of the present study was to prepare noncharged isosters of these compounds, with replacement of the aromatic A ring by a pyridine ring, present in other topoisomerase I inhibitors. Various 7,8- and 8,9-dimethoxy and...

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European Journal of Medicinal Chemistry (8)
Bioorganic & Medicinal Chemistry (6)
Biochemical Pharmacology (3)
Biochemistry (3)
Journal of Medicinal Chemistry (3)
Bioorganic & Medicinal Chemistry Letters (2)
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Chemical Research in Toxicology (1)
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European Journal of Pharmaceutical Sciences (1)
JBIC Journal of Biological Inorganic Chemistry (1)
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INFONA - science communication portal

Search results for: Brigitte Baldeyrou

Synthesis and biological activity of ferrocenyl indeno[1,2-c]isoquinolines as topoisomerase II inhibitors

Synthesis of new biologically active isothiazolo[4,5-b]carbazole-type tetracyclic derivatives via an indole-2,3-quinodimethane approach

Low level of baseline circulating VEGF-A is associated with better outcome in patients with vascular sarcomas receiving sorafenib: an ancillary study from a phase II trial

Synthesis, antiproliferative activity and tubulin targeting effect of acridinone and dioxophenothiazine derivatives

Synthesis of chromeno[3,4-b]indoles as Lamellarin D analogues : A novel DYRK1A inhibitor class

Synthesis, cytotoxicity and topoisomerase inhibition properties of multifarious aminoalkylated indeno[1,2-c]isoquinolin-5,11-diones

Toward new camptothecins. Part 7: Synthesis of thioluotonin and its 5-methoxycarbonyl derivative

Design, Synthesis, and DNA-Binding of N -Alkyl(anilino)quinazoline Derivatives

Indeno[1,2-c]isoquinolin-5,11-diones conjugated to amino acids: Synthesis, cytotoxicity, DNA interaction, and topoisomerase II inhibition properties

Synthesis and biological activities of new furo[3,4-b]carbazoles: Potential topoisomerase II inhibitors

Montmorillonite K-10 catalyzed cyclization of N-ethoxycarbonyl-N′-arylguanidines: Access to pyrimido[4,5-c]carbazole and pyrimido[5,4-b]indole derivatives

Synthesis and antitumoral activity of novel thiazolobenzotriazole, thiazoloindolo[3,2-c]quinoline and quinolinoquinoline derivatives

Synthesis, Cytotoxicity, DNA Interaction, and Topoisomerase II Inhibition Properties of Novel Indeno[2,1- c ]quinolin-7-one and Indeno[1,2- c ]isoquinolin-5,11-dione Derivatives

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

Amino- and glycoconjugates of pyrido[4,3,2-kl]acridine. Synthesis, antitumor activity, and DNA binding

Synthesis of 2,6-diphenylpyrazine derivatives and their DNA binding and cytotoxic properties

Oxoazabenzo[ de ]anthracenes Conjugated to Amino Acids: Synthesis and Evaluation as DNA-Binding Antitumor Agents

Targeting DNA with Novel Diphenylcarbazoles ^†

Novel antitumor indenoindole derivatives targeting DNA and topoisomerase II

Synthesis and cytotoxic activity of benzo[c][1,7] and [1,8]phenanthrolines analogues of nitidine and fagaronine

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