Zobrazeno 1 - 10
of 42
pro vyhledávání: '"DAMIAN GROBELNY"'
Autor:
David K. Chalmers, Jason H. Chaplin, Tina C. Lavranos, Bernard L. Flynn, Annabell F. Leske, Dharam Paul, Gurmit S. Gill, Damian Grobelny, Ernest Hamel, Edmund Kostewicz, Julia Morizzi, M. Katherine Jung, David M. Shackleford, Gabriel Kremmidiotis, Susan A. Charman
Publikováno v:
Journal of Medicinal Chemistry. 54:6014-6027
A structure-activity relationship (SAR) guided design of novel tubulin polymerization inhibitors has resulted in a series of benzo[b]furans with exceptional potency toward cancer cells and activated endothelial cells. The potency of early lead compou
Publikováno v:
International Journal of Peptide and Protein Research. 32:292-297
Nα-(Phenethylphosphono)-l-alanyl-l-proline 1, a potent inhibitor of angiotensin converting enzyme, exhibits two 31P n.m.r. resonances (intensity ratio one to one), which exchange with a constant (k1) of about 1 s−1 and a free energy of activation
Publikováno v:
The Journal of Organic Chemistry. 73:1131-1134
A convenient method for the synthesis of 2-bromo-3-aroyl-benzo[b]furans from readily accessible precursors has been developed. The 2-bromo group has been employed as a versatile synthetic handle in both palladium-mediated couplings and direct nucleop
Publikováno v:
Molecular Simulation. 28:827-843
NMR spectroscopy techniques have been used to determine the conformation of DG35-VIII in DMSO, acetone, and methanol. COSY and Heteronuclear Correlation experiments were used to confirm the proton spectral assignments. NOESY experiments were used to
Autor:
Daniel E. Levy, France Lapierre, Weisheng Liang, Wenqing Ye, Christopher W. Lange, Xiaoyuan Li, Damian Grobelny, Marie Casabonne, David Tyrrell, Kevin Holme, Alex Nadzan, Richard E. Galardy
Publikováno v:
Journal of Medicinal Chemistry. 41:199-223
Modifications around the dipeptide-mimetic core of a hydroxamic acid based matrix metalloproteinase inhibitor were studied. These variations incorporated a variety of natural, unnatural, and synthetic amino acids in addition to modifications of the P
Antiviral Activity of DG-35-VIII, a Potent Inhibitor of the Protease of Human Immunodeficiency Virus
Publikováno v:
Antiviral Chemistry and Chemotherapy. 8:99-106
The protease of human immunodeficiency virus (HIV) is an important target for antiretroviral drug therapy. The synthesis and in vitro antiviral activity of a novel protease inhibitor, DG-35-VIII, which contains an hydroxyethylhydrazide core unit, is
Autor:
RICHARD E. GALARDY, MARIE E. CASSABONNE, CARLANNE GIESE, JAMES H. GILBERT, FRANCE LAPIERRE, HENRY LOPEZ, MARY E. SCHAEFER, ROBERT STACK, MICHAEL SULLIVAN, BRENT SUMMERS, ROB TRESSLER, DAVE TYRRELL, JENNIFER WEE, SCOTT D. ALLEN, JOHN J. CASTELLOT, JOHN P. BARLETTA, GREGORY S. SCHULTZ, LEONARDO A. FERNANDEZ, SUSAN FISHER, TIAN-YI CUI, HARALD G. FOELLMER, DAMIAN GROBELNY, WALTER M. HOLLERAN
Publikováno v:
Annals of the New York Academy of Sciences. 732:315-323
Autor:
Clifford Librach, King Chiu, Susan J. Fisher, Damian Grobelny, Marilyn L. Fitzgerald, Caroline H. Damsky, Richard E. Galardy, Zena Werb, Nanci M. Corwin, Ruth A. Esteves
Publikováno v:
The Journal of Cell Biology
The specialized interaction between embryonic and maternal tissues is unique to mammalian development. This interaction begins with invasion of the uterus by the first differentiated embryonic cells, the trophoblasts, and culminates in formation of t
Publikováno v:
ChemInform. 39
A convenient method for the synthesis of 2-bromo-3-aroyl-benzo[b]furans from readily accessible precursors has been developed. The 2-bromo group has been employed as a versatile synthetic handle in both palladium-mediated couplings and direct nucleop
Publikováno v:
Biochemistry. 31(31)
The hydroxamic acid HONHCOCH2CH(i-Bu)CO-L-Trp-NHMe, isomer 6A (GM 6001), inhibits human skin fibroblast collagenase with Ki of 0.4 nM using the synthetic thiol ester substrate Ac-Pro-Leu-Gly-SCH(i-Bu)CO-Leu-Gly-OEt at pH 6.5. The other isomer, 6B, wh