Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Katherine A, Rouleau"'
Autor:
Sam T. Chao, Yufen Zhao, Katherine A. Rouleau, Zheng Yang, Henry H. Gu, Catherine A. Fleener, Zhongqi Shen, Jeffrey A. Robl, Kim W. McIntyre, Edwin J. Iwanowicz, Mark R. Witmer, Scott H. Watterson, Arvind Mathur, Bang-Chi Chen, Mary T. Obermeier, and Robert Townsend, Donna M. Dambach, T. G. Murali Dhar, Zili Xiao, Joel C. Barrish, Shelley K. Ballentine, David J. Shuster, Ping Chen
Publikováno v:
Journal of Medicinal Chemistry. 50:3730-3742
Inosine monophosphate dehydrogenase (IMPDH), a key enzyme in the de novo synthesis of guanosine nucleotides, catalyzes the irreversible nicotinamide-adenine dinucleotide dependent oxidation of inosine-5'-monophosphate to xanthosine-5'-monophosphate.
Autor:
Robert M. Townsend, Zhongqi Shen, Catherine A. Fleener, Derek J. Norris, Scott H. Watterson, Henry H. Gu, Ping Chen, Diane Hollenbaugh, T. G. Murali Dhar, Joel C. Barrish, Shelley K. Ballentine, Edwin J. Iwanowicz, Katherine A. Rouleau
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3557-3560
A series of novel small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH), based upon a 3-cyanoindole core, were explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, i
Autor:
Catherine A. Fleener, Henry H. Gu, Daniel L. Cheney, Edwin J. Iwanowicz, Robert M. Townsend, Ping Chen, Katherine A. Rouleau, Junqing Guo, T. G. Murali Dhar, William J. Pitts, Diane Hollenbaugh, Scott H. Watterson, Zhongqi Shen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:2059-2063
The first reported structure-activity relationships (SARs) about the N-[3-methoxy-4-(5-oxazolyl)phenyl moiety for a series of recently disclosed inosine monophosphate dehydrogenase (IMPDH) inhibitors are described. The syntheses and in vitro inhibito
Autor:
Edwin J. Iwanowicz, Kristin D. Haslow, Donna A. Bassolino, Derek J. Norris, Robert M. Townsend, Daniel L. Cheney, Joel C. Barrish, William J. Pitts, Scott H. Watterson, Katherine A. Rouleau, Catherine A. Fleener, T. G. Murali Dhar, Diane Hollenbaugh, Ping Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:1345-1348
Screening of our in-house compound collection led to the discovery of 5-bromo-6-amino-2-isoquinoline 1 as a weak inhibitor of IMPDH. Subsequent optimization of 1 afforded a series of novel 2-isoquinolinoaminooxazole-based inhibitors, represented by 1
Autor:
Marianne Carlsen, Daniel L. Cheney, Junqing Guo, John S. Chorba, Robert M. Townsend, Edwin J. Iwanowicz, Henry H. Gu, Mark R. Witmer, Derek J. Norris, Katherine A. Rouleau, Zhongqi Shen, William J. Pitts, Diane Hollenbaugh, Scott H. Watterson, T. G. Murali Dhar, Catherine A. Fleener, Ping Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:543-546
A series of novel quinolone-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are described.
Autor:
Edwin J. Iwanowicz, Henry Gu, N.Z. Sherbina, Joel C. Barrish, T. G. Murali Dhar, Catherine A. Fleener, Katherine A. Rouleau, Chunjian Liu, Junquing Guo, William J. Pitts, Scott H. Watterson, Diane Hollenbaugh
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:3125-3128
A series of heterocyclic replacements for the central diamide moiety of 1, a potent small molecule inhibitor of inosine monophosphate dehydrogenase (IMPDH) were explored The synthesis and the structure-activity relationships (SARs), derived from in v
Autor:
N.Z. Sherbina, Chunjian Liu, Diane Hollenbaugh, Katherine A. Rouleau, Toomas Mitt, Scott H. Watterson, Joel C. Barrish, Katerina Leftheris, Henry H. Gu, Catherine A. Fleener, Edwin J. Iwanowicz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:2931-2934
A series of novel guanidine-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, immunosuppressive an
Autor:
T G Murali, Dhar, Zhongqi, Shen, Junqing, Guo, Chunjian, Liu, Scott H, Watterson, Henry H, Gu, William J, Pitts, Catherine A, Fleener, Katherine A, Rouleau, N Z, Sherbina, Kim W, McIntyre, David J, Shuster, Mark R, Witmer, Jeffrey A, Tredup, Bang-Chi, Chen, Rulin, Zhao, Mark S, Bednarz, Daniel L, Cheney, John F, MacMaster, Laura M, Miller, Karen K, Berry, Timothy W, Harper, Joel C, Barrish, Diane L, Hollenbaugh, Edwin J, Iwanowicz
Publikováno v:
Journal of Medicinal Chemistry. 45:2127-2130
Inosine monophosphate dehydrogenase (IMPDH) is a key enzyme that is involved in the de novo synthesis of purine nucleotides. Novel 2-aminooxazoles were synthesized and tested for inhibition of IMPDH catalytic activity. Multiple analogues based on thi
Autor:
Philip M. Wallace, John F. MacMaster, Katherine A. Rouleau, T. Joseph Brown, James K. Loy, Karen L. Donaldson, Alan F. Wahl
Publikováno v:
The Journal of Immunology. 162:5547-5555
Oncostatin M (OM) is a pleiotropic cytokine produced late in the activation cycle of T cells and macrophages. In vitro it shares properties with related proteins of the IL-6 family of cytokines; however, its in vivo properties and physiological funct
Autor:
Daniel L. Cheney, Diane Hollenbaugh, Robert M. Townsend, Scott H. Watterson, Shelley K. Ballentine, Joel C. Barrish, Katherine A. Rouleau, Edwin J. Iwanowicz, Zhongqi Shen, Catherine A. Fleener, T. G. Murali Dhar
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(7)
The development of a series of novel indole-based inhibitors of 5'-inosine monophosphate dehydrogenase (IMPDH) is described. Various hydrogen bond acceptors at C-3 of the indole were explored. The synthesis and the structure-activity relationships (S