Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Michael D. Boisclair"'
Autor:
Steven P. Seitz, Sarah Cox, Pieter F. W. Stouten, Michael D. Boisclair, Stephen L. Brenner, Jay A. Markwalder, Karen A. Rossi, Leonardo Brizuela, Chong-Hwan Chang
Publikováno v:
Journal of Computer-Aided Molecular Design. 19:111-122
Cyclin-dependent kinases (CDKs) play a key role in regulating the cell cycle. The cyclins, their activating agents, and endogenous CDK inhibitors are frequently mutated in human cancers, making CDKs interesting targets for cancer chemotherapy. Our ai
Autor:
Jie Liu, John F. Boylan, Chong-Hwan Chang, Thais M. Sielecki, Haiying Chen, Robert H. Grafstrom, Angela Smallwood, Catherine R. Burton, Michael D. Boisclair, Steven P. Seitz, Tricia L. Johnson, Sarah Cox, George L. Trainor, Pamela A. Benfield, Jodi K. Muckelbauer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1157-1160
Quinazolines have been identified as inhibitors of CDK4/D1 and CDK2/E. Aspects of the SAR were investigated using solution-phase, parallel synthesis. An X-ray crystal structure was obtained of quinazoline 51 bound in CDK2 and key interactions within
Autor:
Peter J. Worland, Christopher McClure, Muzammil M. Mansuri, Krishna K. Murthi, Marja Dubay, Leonardo Brizuela, Kollol Pal, Michael D. Boisclair
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:1037-1041
Cyclin dependent kinases (CDKs) along with the complementary cyclins form key regulatory checkpoint controls on the cell cycle. Flavopiridol is a synthetic flavone that shows potent and selective cyclin-dependent kinase inhibitory activity. In this p
Autor:
David Epstein, Gustave Bergnes, Carla L. Gilliam, Katharine V. Blake, Kollol Pal, Michael D. Boisclair, Jill Blanchard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:2849-2854
The four-component Ugi reaction was utilized to prepare a library of dipeptidic compounds in order to explore the binding requirements of the key cell cycle phosphatase, Cdc25. Several phosphate surrogates were incorporated into the Ugi product to mi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2015-2020
Analogs of sulfircin (1) were synthesized and tested for inhibitory activity against a panel of phosphatases. We attempted to optimize the potency and selectivity of sulfircin for Cdc25A by modifying three structural areas of the molecule. An anionic
Publikováno v:
ChemInform. 28
Autor:
David Epstein, Carla L. Gilliam, Katharine V. Blake, Kollol Pal, Michael D. Boisclair, Jill Blanchard, Gustave Bergnes
Publikováno v:
ChemInform. 31
The four-component Ugi reaction was utilized to prepare a library of dipeptidic compounds in order to explore the binding requirements of the key cell cycle phosphatase, Cdc25. Several phosphate surrogates were incorporated into the Ugi product to mi
Autor:
Leonardo Brizuela, Krishna K. Murthi, Peter J. Worland, Marja Dubay, Kollol Pal, Michael D. Boisclair, Christopher McClure, Muzammil M. Mansuri
Publikováno v:
ChemInform. 31
Cyclin dependent kinases (CDKs) along with the complementary cyclins form key regulatory checkpoint controls on the cell cycle. Flavopiridol is a synthetic flavone that shows potent and selective cyclin-dependent kinase inhibitory activity. In this p
Autor:
Sarah Cox, Michael D. Boisclair, Charity L. Dean, Philip M. Czerniak, Pieter F. W. Stouten, David A. Nugiel, Steven P. Seitz, Chong-Hwan Chang, Catherine R. Burton, Marc R. Arnone, Lisa M. Sisk, Robert F. Kaltenbach, Barbara A. Harrison, Pamela A. Benfield, Robert H. Grafstrom, Jay A. Markwalder, Susan R. Sherk, Karen A. Rossi, Deborah Doleniak, Peter Worland, George L. Trainor
Publikováno v:
Journal of medicinal chemistry. 47(24)
Using a high-throughput screening strategy, a series of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-ones was identified that inhibit the cyclin-dependent kinase (CDK) 4/cyclin D1 complex-mediated phosphorylation of a protein substrate with IC(50
Autor:
Jie Liu, Robert H. Grafstrom, George L. Trainor, Kimberly Harrison, Diane M. Sharp, Jay A. Markwalder, David J. Carini, Yuki Nakano, Emeka Akamike, Pamela A. Benfield, Sarah Cox, John F. Boylan, Robert F. Kaltenbach, Catherine R. Burton, Thais M. Sielecki, Michael D. Boisclair, Steven P. Seitz, Barbara A. Harrison, Leonardo Brizuela
Publikováno v:
Bioorganicmedicinal chemistry letters. 11(16)
A new structural type of kinase inhibitor, containing a benzocarbazole nucleus, has been identified. Members of the series are selective for inhibition of the cyclin dependent kinase family of enzymes. Although the cdks are highly homologous, represe