ANIMAL CELL;
ANIMAL EXPERIMENT;
ANTINEOPLASTIC ACTIVITY;
ANTIPROLIFERATIVE ACTIVITY;
ARTICLE;
CONTROLLED STUDY;
DRUG POTENCY;
DRUG SCREENING;
DRUG SYNTHESIS;
FEMALE;
HUMAN;
HUMAN CELL;
IC 50;
IN VIVO STUDY;
MOUSE;
NONHUMAN;
QUANTITATIVE ANALYSIS;
STRUCTURE ACTIVITY RELATION;
TUMOR XENOGRAFT;
Activation of Glycogen Synthase Kinase-3 Induces Alzheimer-like Tau Hyperphosphorylation in Rat Hippocampus Slices in Culture
Li, X.; Lu, F.; Tian, Q.; Yang, Y.; Wang, Q.; Wang, J. Z. Activation of Glycogen Synthase Kinase-3 Induces Alzheimer-like Tau Hyperphosphorylation in Rat Hippocampus Slices in Culture J. Neural Transm. 2006, 113, 93-102
Flavopiridol, the First Cyclin-Dependent Kinase Inhibitor: Recent Advances in Combination Chemotherapy
Wang, L. M.; Ren, D. M. Flavopiridol, the First Cyclin-Dependent Kinase Inhibitor: Recent Advances in Combination Chemotherapy Mini Rev. Med. Chem. 2010, 11, 1058-1070
Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin- 5-yl](2,3-difluoro-6-methoxy phenyl)methanone (R547), a Potent and Selective Cyclin-Dependent Kinase Inhibitor with Significant in Vivo Antitumor Activity
Chu, X. J.; De Pinto, W.; Bartkovitz, D.; So, S. S.; Vu, B. T.; Packman, K.; Lukacs, C.; Ding, Q.; Jiang, N.; Wang, K.; Goelzer, P.; Yin, X.; Smith, M. A.; Higgins, B. X.; Chen, Y.; Xiang, Q.; Moliterni, J.; Kaplan, G.; Graves, B.; Lovey, A.; Fotouhi, N. Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4- ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxy phenyl)methanone (R547), a Potent and Selective Cyclin-Dependent Kinase Inhibitor with Significant in Vivo Antitumor Activity J. Med. Chem. 2006, 49, 6549-6560
Phase I and Pharmacologic Study of SNS-032, a Potent and Selective Cdk 2, 7, and 9 Inhibitor, in Patients with Advanced Chronic Lymphocytic Leukemia and Multiple Myeloma
Tong, W. G.; Chen, R.; Plunkett, W.; Siegel, D.; Sinha, R.; Harvey, R. D.; Badros, A. Z.; Popplewell, L.; Coutre, S.; Fox, J. A.; Mahadocon, K.; Chen, T.; Kegley, P.; Hoch, U.; Wierda, W. G. Phase I and Pharmacologic Study of SNS-032, a Potent and Selective Cdk 2, 7, and 9 Inhibitor, in Patients with Advanced Chronic Lymphocytic Leukemia and Multiple Myeloma J. Clin. Oncol. 2010, 18, 3015-3022
A Novel Orally Active Small Molecule Potently Induces G1 Arrest in Primary Myeloma Cells and Prevents Tumour Growth by Specific Inhibition of Cyclin-Dependent Kinase 4/6
Baughn, L. B.; Di Liberto, M.; Wu, K.; Toogood, P. L.; Louie, T.; Gottschalk, R.; Niesvizky, R.; Cho, H.; Ely, S.; Moore, M. A.; Chen-Kiang, S. A Novel Orally Active Small Molecule Potently Induces G1 Arrest in Primary Myeloma Cells and Prevents Tumour Growth by Specific Inhibition of Cyclin-Dependent Kinase 4/6 Cancer Res. 2006, 66, 7661-7667
AZD5438, a Potent Oral Inhibitor of Cyclin-Dependent Kinases 1, 2, and 9, Leads to Pharmacodynamic Changes and Potent Antitumor Effects in Human Tumor Xenografts
Byth, K. F.; Thomas, A.; Hughes, G.; Forder, C.; Mc Gregor, A.; Geh, C.; Oakes, S.; Green, C.; Walker, M.; Newcombe, N.; Green, S.; Growcott, J.; Barker, A.; Wilkinson, R. W. AZD5438, a Potent Oral Inhibitor of Cyclin-Dependent Kinases 1, 2, and 9, Leads to Pharmacodynamic Changes and Potent Antitumor Effects in Human Tumor Xenografts Mol. Cancer Ther. 2009, 7, 1856-1866
Toxicity and Toxicokinetics of the Cyclin-Dependent Kinase inhibitor AG-024322 in Cynomolgus Monkeys Following Intravenous infusion
Brown, A. P.; Courtney, C. L.; Criswell, K. A.; Holliman, C. L.; Evering, W.; Jessen, B. A. Toxicity and Toxicokinetics of the Cyclin-Dependent Kinase inhibitor AG-024322 in Cynomolgus Monkeys Following Intravenous infusion Cancer Chemother. Pharmacol. 2008, 62, 1091-1101
Identification of N -(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1 H -pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design
Wyatt, P. G.; Woodhead, A. J.; Berdini, V.; Boulstridge, J. A.; Carr, M. G.; Cross, D. M.; Davis, D. J.; Devine, L. A.; Early, T. R.; Feltell, R. E.; Lewis, E. J.; McMenamin, R. L.; Navarro, E. F.; O'Brien, M. A.; O'Reilly, M.; Reule, M.; Saxty, G.; Seavers, L. C.; Smith, D. M.; Squires, M. S.; Trewartha, G.; Walker, M. T.; Woolford, A. J. Identification of N -(4-Piperidinyl)-4-(2,6- dichlorobenzoylamino)-1 H -pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design J. Med. Chem. 2008, 51, 4986-4999
Enzastaurin Shows Preclinical Antitumor Activity against Human Transitional Cell Carcinoma and Enhances the Activity of Gemcitabine
Jian, W.; Yamashita, H.; Levitt, J. M.; Lerner, S. P.; Sonpavde, G. Enzastaurin Shows Preclinical Antitumor Activity against Human Transitional Cell Carcinoma and Enhances the Activity of Gemcitabine Mol. Cancer Ther. 2009, 8, 1772-1778
New Efficient Access to Fused Aryltetrahydroindolizinones via N -Acyliminium Intermediates
Chiurato, M.; Routier, S.; Troin, Y.; Guillaumet, G. New Efficient Access to Fused Aryltetrahydroindolizinones via N -Acyliminium Intermediates Eur. J. Org. Chem. 2009, 18, 3011-3021
New Efficient Access to Fused (Het)aryltetrahydroindolizinones via N -Acyl Iminium Intermediates
Chiurato, M.; Routier, S.; Troin, Y.; Guillaumet, G. New Efficient Access to Fused (Het)aryltetrahydroindolizinones via N -Acyl Iminium Intermediates Tetrahedron 2010, 66, 4647-4653
Structure-Based Generation of a New Class of Potent Cdk4 Inhibitors: New de Novo Design Strategy and Library Design
Honma, T.; Hayashi, Y.; Aoyama, T.; Hashimoto, N.; Machida, T.; Fukasawa, K.; Iwama, T.; Ikeura, C.; Ikuta, M.; Suzuki-Takahashi, I.; Iwasawa, Y.; Hayama, T.; Nishimura, S.; Morishima, H. Structure-Based Generation of a New Class of Potent Cdk4 Inhibitors: New de Novo Design Strategy and Library Design J. Med. Chem. 2001, 44, 4615-4627
A Novel Approach for the Development of Selective Cdk4 Inhibitors: Library Design Based on Locations of Cdk4 Specific Amino Acid Residues
Honma, T.; Yoshizumi, T.; Hashimoto, N.; Hayashi, K.; Kawanishi, K.; Fukasawa, K.; Takaki, T.; Ikeura, C.; Ikuta, M.; Suzuki-Takahashi, I.; Hayama, T.; Nishimura, S.; Morishima, H. A Novel Approach for the Development of Selective Cdk4 Inhibitors: Library Design Based on Locations of Cdk4 Specific Amino Acid Residues J. Med. Chem. 2001, 44, 4628-4640
Short Diastereoselective Synthesis of cis - And trans -Hexahydropyrido[2,1-a]isoindole Derivatives
Alsarabi, A.; Canet, J. L.; Troin, Y. Short Diastereoselective Synthesis of cis-and trans -Hexahydropyrido[2,1-a]isoindole Derivatives Tetrahedron Lett. 2004, 45, 9003-9006
Routier, S.; Guillaumet, G.; Meijer, L.; Chiurato, M.; Boulahjar, R. 10-Amino-1,2,3,4-tetrahydropyrido[2,1-a]isoindol-6(10bH)-ones as CDK1, 5 and GSK-3 inhibitors. Patent WO 201050416
Use of Chloroalkenylamines for the Synthesis of 1-Azabicyclo[3.3.0]octane and 1-Azabicyclo[4.3.0]nonane Derivatives
Lochead, A. W.; Proctor, G. R.; Caton, M. P. L. Use of Chloroalkenylamines for the Synthesis of 1-Azabicyclo[3.3.0]octane and 1-Azabicyclo[4.3.0]nonane Derivatives J. Chem. Soc., Perkin Trans. 1 1984, 2477-2489
Brown, A. D.; Ellis, D.; Smith, C. R., Substituted Triazole Derivatives As Oxytocin Antagonists Their Preparation and Use against Sexual Dysfunction. Patent WO2005028452
Novel Bis(indolyl)maleimide Pyridinophosphanes That Are Potent, Selective Inhibitors of Glycogen Synthase Kinase-3
Zhang, H. C.; Boñaga, L. V. R.; Ye, H.; Derian, C. K.; Damiano, B. P.; Maryanoff, B. E. Novel Bis(indolyl)maleimide Pyridinophosphanes That Are Potent, Selective Inhibitors of Glycogen Synthase Kinase-3 Bioorg. Med. Chem. Lett. 2007, 17, 2863-2868
Leucettines, a Class of Potent Inhibitors of cdc2-like Kinases and Dual Specificity, Tyrosine Phosphorylation Regulated Kinases Derived from the Marine Sponge Leucettamine B. Modulation of Alternative Pre-RNA Splicing
Debdab, M.; Carreaux, F.; Renault, S.; Soundararajan, M.; Fedorov, O.; Filippakopoulos, P.; Lozach, O.; Babault, L.; Tahtouh, T.; Baratte, B.; Ogawa, Y.; Hagiwara, M.; Eisenreich, A.; Rauch, U.; Knapp, S.; Meijer, L.; Bazureau, J.-P. Leucettines, a Class of Potent Inhibitors of cdc2-like Kinases and Dual Specificity, Tyrosine Phosphorylation Regulated Kinases Derived from the Marine Sponge Leucettamine B. Modulation of Alternative Pre-RNA Splicing J. Med. Chem. 2011, 54, 4172-4186
Indirubins Inhibit Glycogen Synthase Kinase - 3 β and CDK5/p25, Two Kinases Involved in Abnormal Tau Phosphorylation in Alzheimer's Disease - A Property Common to Most CDK Inhibitors?
Leclerc, S.; Garnier, M.; Hoessel, R.; Marko, D.; Bibb, J. A.; Snyder, G. L.; Greengard, P.; Biernat, J.; Mandelkow, E.-M.; Eisenbrand, G.; Meijer, L. Indirubins Inhibit Glycogen Synthase Kinase-3 β and CDK5/p25, Two Kinases Involved in Abnormal Tau Phosphorylation in Alzheimer's Disease-A Property Common to Most CDK Inhibitors? J. Biol. Chem. 2001, 276, 251-260
Purification of GSK-3 by Affinity Chromatography on Immobilised Axin
Primot, A.; Baratte, B.; Gompel, M.; Borgne, A.; Liabeuf, S.; Romette, J. L.; Costantini, F.; Meijer, L. Purification of GSK-3 by Affinity Chromatography on Immobilised Axin Protein Expr. Purif. 2000, 20, 394-404
