Výsledky vyhledávání - "Philippe Schambel"

Plant natural fragments, an innovative approach for drug discovery

Autor: Philippe Schambel, Antonio Grondin, Denis Zeyer, Bruno David, Marc Vitorino

Publikováno v: Phytochemistry Reviews. 19:1141-1156

Plant natural products (PNP) (e.g., secondary vegetal metabolites and their derivatives) have been a productive source of active ingredients for the pharmaceutical industry. The High Throughput Screening of Plant Natural Products (PNP-HTS) with extra

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::976a7545d9e933ad9c95c801cc46adb5
https://doi.org/10.1007/s11101-019-09612-4

Zobrazit plný text záznamu

Identification and optimization of hydrazone-gallate derivatives as specific inhibitors of DNA methyltransferase 3A

Autor: Yoann Menon, Christina Gros, Philippe Schambel, Véronique Masson, Paola B. Arimondo, Alexandre Erdmann, Yannick Aussagues, Michel Baltas, Frédéric Ausseil, Natacha Novosad

Publikováno v: Future Medicinal Chemistry
Future Medicinal Chemistry, 2016, 8 (4), pp.373-380. ⟨10.4155/fmc.15.192⟩
Future Medicinal Chemistry, Future Science, 2016, 8 (4), pp.373-380. ⟨10.4155/fmc.15.192⟩

DNA methylation is the most studied epigenetic event. Since the methylation profile of the genome is widely modified in cancer cells, DNA methyltransferases are the target of new anticancer therapies. Nucleosidic inhibitors suffer from toxicity and c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a6efa7f1c8834da3dc665ef3e4cc34a
https://doi.org/10.4155/fmc.15.192

Zobrazit plný text záznamu

From pure FPP to mixed FPP and CAAX competitive inhibitors of farnesyl protein transferase

Autor: Marie Lamothe, Bridget T. Hill, Michel Perez, Chantal Etievant, Marc Lannuzel, Philippe Schambel

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:1459-1462

Starting from a FPP analogue with nanomolar inhibitory activity against isolated FPTase, yet lacking activity in cellular assays, structural modifications were performed to enhance cellular activity by removing all acidic functionalities. Overall, th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f019124302b11f28e41db4d2a3d09a4
https://doi.org/10.1016/s0960-894x(03)00171-9

Zobrazit plný text záznamu

Synthesis and evaluation of a novel series of farnesyl protein transferase inhibitors as non-peptidic CAAX tetrapeptide analogues

Autor: Michel Perez, Marie Lamothe, Philippe Schambel, Catherine Maraval, Bridget T. Hill, Chantal Etievant, Stephan Dumond

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:1455-1458

A novel series of compounds, derived from 4-amino-phenyl piperazine, has been designed to selectively inhibit farnesyl protein transferase (FPTase) as CAAX tetrapeptide analogues. Certain of these compounds were shown to possess low nanomolar inhibit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ad62269f659d225841bf11bbdf44d01d
https://doi.org/10.1016/s0960-894x(03)00170-7

Zobrazit plný text záznamu

Design, synthesis and biological evaluation of 4-amino-N- (4-aminophenyl)benzamide analogues of quinoline-based SGI-1027 as inhibitors of DNA methylation

Autor: Philippe Schambel, Arumugam Rajavelu, Jean-Marc Gregoire, Alexandre Erdmann, François Sautel, Elodie Rilova, Véronique Masson, Paola B. Arimondo, Stéphane Vispé, Yoann Menon, Christina Gros, Natacha Novosad, Valérie Poughon-Cassabois, Frédéric Cantagrel, Yannick Aussagues, Albert Jeltsch, Frédéric Ausseil

Publikováno v: Chemmedchem

Quinoline derivative SGI-1027 (N-(4-(2-amino-6-methylpyrimidin-4-ylamino)phenyl)-4-(quinolin-4-ylamino)benzamide) was first described in 2009 as a potent inhibitor of DNA methyltransferase (DNMT) 1, 3A and 3B. Based on molecular modeling studies, per

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d863bc2797c728efd7828a4b7ea7b7b
https://pubmed.ncbi.nlm.nih.gov/24678024

Zobrazit plný text záznamu

Synthesis and Evaluation of Analogues of N-Phthaloyl-L-tryptophan (RG108) as Inhibitors of DNA Methyltransferase 1

Autor: Alexandre Ceccaldi, Philippe Schambel, Catherine Senamaud-Beaufort, Thierry Drujon, Christine Champion, Philippe Karoyan, Paola B. Arimondo, Gaël Marloie, Dominique Guianvarc'h, Saâdia Asgatay, Arumugam Rajavelu, Alexandre Erdmann, Olivier Lequin, Albert Jeltsch

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, American Chemical Society, 2013, 57 (2), pp.421-434. ⟨10.1021/jm401419p⟩
Journal of Medicinal Chemistry, 2013, 57 (2), pp.421-434. ⟨10.1021/jm401419p⟩

International audience; : DNA methyltransferases (DNMT) are promising drug targets in cancer provided that new, more specific, and chemically stable inhibitors are discovered. Among the non-nucleoside DNMT inhibitors, N-Phthaloyl-L-tryptophan 1 (RG10

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd0452e3b2b46d795a16ee9931438d23
https://hal.archives-ouvertes.fr/hal-00920710

Zobrazit plný text záznamu

Meroterpenes from Dichrostachys cinerea inhibit protein farnesyl transferase activity

Autor: Philippe Schambel, Min Gao, Frédéric Ausseil, Georges Massiot, Christophe Menendez, Bruno David, Marie-France Laroche, Christophe Long, Roselyne Raux, Christelle Gau, Catherine Lavaud, Laurence Marcourt, Clément Delaude

Publikováno v: Journal of natural products. 72(10)

Eighteen new meroterpene derivatives, dichrostachines A-R (1-18), have been isolated from the root and stem barks of Dichrostachys cinerea, and their structures determined by spectroscopic means and molecular modeling. From a biosynthetic standpoint

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ad6d6ef157299eaa8e93e02b39a44cb
https://pubmed.ncbi.nlm.nih.gov/19761234

Zobrazit plný text záznamu

Differentiation between partial agonists and neutral 5-HT1B antagonists by chemical modulation of 3-[3-(N,N-dimethylamino)propyl]-4-hydroxy- N-[4-(pyridin-4-yl)phenyl]benzamide (GR-55562)

Autor: Philippe Schambel, Karine Belliard, Serge Halazy, Petrus J. Pauwels, Marie Lamothe

Publikováno v: Journal of medicinal chemistry. 40(22)

The synthesis and binding affinity at cloned h5-HT1D, h5-HT1D, and h5-HT1A receptors of 3-[3-(N,N-dimethylamino)propyl]-4-hydroxy- N-[4-(pyridin-4-yl)phenyl]benzamide (2, GR-55562) and four O-methylated analogs are described. The functional activity

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02eee21ca0ed5587fb5464ed367b294f
https://pubmed.ncbi.nlm.nih.gov/9357521

Zobrazit plný text záznamu

Binding of arylpiperazines, (aryloxy)propanolamines, and tetrahydropyridylindoles to the 5-HT1A receptor: contribution of the molecular lipophilicity potential to three-dimensional quantitative structure-affinity relationship models

Autor: Patrick Gaillard, Bernard Testa, Pierre-Alain Carrupt, Philippe Schambel

Publikováno v: Journal of Medicinal Chemistry, Vol. 39, No 1 (1996) pp. 126-134

A set of 280 5-HT1A receptor ligands were selected from available literature data according to predefined criteria and subjected to three-dimensional quantitative structure-affinity relationship analysis using comparative molecular field analysis. No

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f08689c5550a0026830f44958e5deea
https://pubmed.ncbi.nlm.nih.gov/8568799

Zobrazit plný text záznamu

An improved synthesis of 18-norandrost-4-ene-3,17-dione

Autor: Elisabeth Davioud, Philippe Schambel, Andrée Marquet, Antoinette Viger

Publikováno v: Steroids. 58(3)

We describe the synthesis of 13β- and 13α-H-18-nor-androst-4-ene-3,17-dione ( 1a and 1b ) from 18-hydroxyprogesterone (18 → 20) hemiketal, via the 18-acetoxy-17β-hydroxyandrost-4-en-3-one formed by a modified Baeyer-Villiger reaction. Saponifica

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::48ace3713d041515b4ad2dc6b7b2f186
https://pubmed.ncbi.nlm.nih.gov/8475519

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání