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5 results on '"Stéphanie Blanchard"'

1. DIHYDRODIPYRIDOPYRAZINES: SYNTHESIS AND FUNCTIONALIZATION

Author

Gérald Guillaumet, Adriana Fînaru, Oana-Irina Patriciu, Stéphanie Blanchard, and Irina Grig-Alexa

Subjects
dihydrodipyridopyrazines, hetarynic cyclization, Pd catalysis, Alkylation, reduction, Cyclization, Smiles rearrangement, dipyridinylamines, Chemical technology, TP1-1185
Abstract

Different conceptual synthetic approaches to the elaboration of a new family of planar polynuclear nitrogen containing aromatic heterocycles – the dihydrodipyridopyrazines – are reviewed: the arynic reaction, the sequence palladium coupling reaction - substitution - reduction - cyclization - substitution or through the intermediacy of Smiles rearrangement. Further functionalization of these compounds by substitution reaction, metalation sequence and palladium-catalyzed coupling reaction are also discussed.

Published
2010

2. 2-Anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1

Author

Chang Kai Soh, Kay Lin Goh, Meredith Williams, Kantharaj Ethirajulu, Haishan Wang, Zahid Bonday, Jeanette Marjorie Wood, Miah Kiat Goh, Kee Chuan Goh, Brian Dymock, Anders Poulsen, Stéphanie Blanchard, Mohammed Khalid Pasha, and Chai Ping Lee

Subjects
Clinical Biochemistry, Pharmaceutical Science, Protein Serine-Threonine Kinases, Pharmacology, Biochemistry, Small Molecule Libraries, Inhibitory Concentration 50, Mice, Cell Line, Tumor, Drug Discovery, Animals, Humans, Enzyme Inhibitors, Molecular Biology, Protein kinase B, Cells, Cultured, PI3K/AKT/mTOR pathway, ADME, Aniline Compounds, Molecular Structure, biology, Kinase, Cell growth, Akt/PKB signaling pathway, Chemistry, Organic Chemistry, Cyclin-dependent kinase 2, Pyruvate Dehydrogenase Acetyl-Transferring Kinase, Enzyme Activation, Solubility, Purines, Cancer cell, biology.protein, Molecular Medicine
Abstract

A series of 2-anilino substituted 4-aryl-8H-purines were prepared as potent inhibitors of PDK1, a serine-threonine kinase thought to play a role in the PI3K/Akt signaling pathway, a key mediator of cancer cell growth, survival and tumorigenesis. The synthesis, SAR and ADME properties of this series of compounds are discussed culminating in the discovery of compound 6 which possessed sub-micromolar cell proliferation activity and 65% oral bioavailability in mice.

Published
2012
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3. Synthesis and evaluation of alkenyl indazoles as selective Aurora kinase inhibitors

Author

Anders Poulsen, Kee Chuan Goh, Ee Ling Teo, Chee Pang Ng, Stéphanie Blanchard, Evelyn Tan, Wai Chung Ong, Kay Lin Goh, Weiping Deng, Angeline C.-H. Lee, Eric T. Sun, Anthony D. William, Noah Tu, and Zahid Bonday

Subjects
Models, Molecular, Subfamily, Stereochemistry, Clinical Biochemistry, Drug Evaluation, Preclinical, Pharmaceutical Science, macromolecular substances, Protein Serine-Threonine Kinases, Biochemistry, chemistry.chemical_compound, Aurora kinase, Aurora Kinases, Drug Discovery, Protein Kinase Inhibitors, Molecular Biology, Indazole, biology, Chemistry, Organic Chemistry, Enzyme assay, enzymes and coenzymes (carbohydrates), embryonic structures, biology.protein, Molecular Medicine, biological phenomena, cell phenomena, and immunity, Selectivity
Abstract

A series of alkenyl indazoles were synthesized and evaluated in Aurora kinase enzyme assays. Several promising leads were optimized for selectivity towards Aurora B. Excellent binding affinity and good selectivity were achieved with optimized compounds in isolated Aurora subfamily assays.

Published
2010
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4. N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: Design, synthesis, SAR studies, and in vivo antitumor activity

Author

Hong Yan Song, Melvin Ng, Zou Yong, Eric T. Sun, Michael Entzeroth, Anders Poulsen, Dizhong Chen, Kee Chuan Goh, Joyce Wei Wei Chang, Kanda Sangthongpitag, Walter Stünkel, Niefang Yu, Zahid Bonday, Haishan Wang, Weiping Deng, Lye Pek Ling, Stéphanie Blanchard, Hwee Hoon Khng, Wai Chung Ong, Lijuan Fang, Xiaofeng Wu, Xukun Wang, and Siok Kun Goh

Subjects
Benzimidazole, Ethylene, Stereochemistry, Clinical Biochemistry, Mice, Nude, Pharmaceutical Science, Antineoplastic Agents, Crystallography, X-Ray, Biochemistry, Histone Deacetylases, Mice, Structure-Activity Relationship, chemistry.chemical_compound, In vivo, Cell Line, Tumor, Drug Discovery, Animals, Humans, Structure–activity relationship, Molecular Biology, chemistry.chemical_classification, Acrylamides, Hydroxamic acid, Organic Chemistry, HCT116 Cells, Xenograft Model Antitumor Assays, Histone Deacetylase Inhibitors, Enzyme, chemistry, Cell culture, Molecular Medicine, Benzimidazoles, Female, Histone deacetylase, Drug Screening Assays, Antitumor
Abstract

A series of N-hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides were designed and synthesized as novel HDAC inhibitors. General SAR has been established for the substituents at positions 1 and 2, as well as the importance of the ethylene group and its attachment to position 5. Optimized compounds are much more potent than SAHA in both enzymatic and cellular assays. A representative compound, 23 (SB639), has demonstrated antitumor activity in a colon cancer xenograft model.

Published
2009
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5. Hetarynic synthesis and chemical transformation of dihydrodipyridopyrazines

Author

Catherine Kuehm-Caubère, Stéphanie Blanchard, Pfeiffer Bruno, Paul Caubere, Gérald Guillaumet, Ivan Rodriguez, and Pierre Renard

Subjects
Chemical transformation, chemistry.chemical_compound, Chemistry, Nitration, Organic Chemistry, Drug Discovery, Organic chemistry, Base (exponentiation), Biochemistry, Formylation
Abstract

Unprecedented dihydrodipyridopyrazines were easily obtained by hetarynic dimerization of 2-alkylamino-3-halogenopyridines in the presence of the complex base NaNH2–tBuONa. Derivatizations of the new heterocycles are described. The anticancer activity of these compounds is also mentioned.

Published
2002
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