Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Lee S. Chong"'
Autor:
William C. Groutas, Radhika Venkataraman, Shu He, Yue He Li, Tien M. Truong, Qinghong Fu, Hongyi Yu, Nga T. Vu, Rongze Kuang, Juan Tu, Lee S. Chong, Sumei Ruan, Jeffrey B. Epp
Publikováno v:
Archives of Biochemistry and Biophysics. 385:162-169
The 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold (I) embodies a motif that allows it to dock to the active site of (chymo)trypsin-like proteases in a predictable and substrate-like fashion. Consequently, inhibitors derived from this heterocyclic s
Autor:
Lee S. Chong, Nadene Houser-Archield, Jeffrey B. Epp, Radhika Venkataraman, Rongze Kuang, He Huang, William C. Groutas, John R. Hoidal
Publikováno v:
Archives of Biochemistry and Biophysics. 332:335-340
Amino acid-derived phthalimide and saccharin derivatives have been investigated for their inhibitory activity toward the serine proteinases human leukocyte elastase, cathepsin G, and proteinase 3. The saccharin derivatives were found to be effective
Asymmetric Synthesis of Calyculin C. 2. Synthesis of the C26−C37 Fragment and Model Wittig Couplings
Autor:
John E. Tellew, John Demattei, Gerard R. Scarlato, Anthony K. Ogawa, Lee S. Chong, Robert W. Armstrong
Publikováno v:
The Journal of Organic Chemistry. 61:6153-6161
We report our synthesis of the C(26)-C(37) fragment of serine/threonine protein phosphatase PP1 and PP2A inhibitor calyculin C (1). Outlined in this paper are synthetic approaches to the two components based on disconnection at the C(33)-N(3) amide b
Autor:
Lee S. Chong, Jeffrey B. Epp, Nadene Houser-Archield, Rongze Kuang, Radhika Venkataraman, John R. Hoidal, William C. Groutas
Publikováno v:
Bioorganic & Medicinal Chemistry. 3:187-193
The results of a structure-activity relationship study focusing on the interaction of a series of phthalimide and saccharin derivatives with leukocyte elastase, cathepsin G and proteinase 3 are described. The phthalimide derivatives were found to be
Autor:
Eun-Hong Kim, Lee S. Chong, Radhika Venkataraman, Michael A. Stanga, Jeffrey B. Epp, William C. Groutas, James E. Yoder
Publikováno v:
Bioorganic & Medicinal Chemistry. 3:125-128
A series of isoxazoline derivatives were synthesized and investigated for their in vitro inhibitory activity towards human leukocyte elastase, cathepsin G and proteinase 3.
Autor:
Lee S. Chong, Radhika Venkataraman, Jeffrey B. Epp, He Huang, Rongze Kuang, William C. Groutas
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:2745-2750
A general approach toward the design of mechanism-based inhibitors of serine proteinases involving the linking of fragment -CHX-COOR to an appropriate recognition element is described.
Publikováno v:
Biochemical and Biophysical Research Communications. 197:730-739
A series of heterocydic compounds designed to function as mechanism-based inhibitors of human leukocyte elastase and cathepsin G has been synthesized and their inhibitory activity was investigated. These isothiazolidin-3-one derivatives were found to
Autor:
Radhika Venkataraman, William C. Groutas, He Huang, Jeffrey B. Epp, Lee S. Chong, Nadene Houser-Archield, Jerald J. McClenahan
Publikováno v:
Journal of Medicinal Chemistry. 36:3178-3181
A series of saccharin derivatives I has been synthesized and evaluated for their inhibitory activity toward human leukocyte elastase and cathepsin G. Most of the compounds were found to be efficient and time-dependent inhibitors of elastase. Inactiva
Autor:
Michael A. Stanga, Jeffrey B. Epp, Lee S. Chong, William C. Groutas, Jerald J. McClenahan, Radhika Venkataraman, Michael J. Brubaker, F. Tagusagawa
Publikováno v:
Biochimica et Biophysica Acta (BBA) - Protein Structure and Molecular Enzymology. 1164:283-288
A series of 3-( alkylthio )-N- hydroxysuccinimide derivatives was synthesized and their inhibitory activity towards human leukocyte elastase (HLE) was investigated. The interaction of the compounds having a 3-alkylthioether side chain (compounds 1 an
Autor:
Radhika Venkataraman, He Huang, Nadene Houser-Archield, Lee S. Chong, Jeffrey B. Epp, Jerald J. McClenahan, Rongze Kuang, Michael J. Brubaker, William C. Groutas
Publikováno v:
Biochemical and Biophysical Research Communications. 194:1491-1499
Neutrophil-derived mediators such as, for example, the serine proteinase elastase, cathepsin G and proteinase 3, play a critical role in inflammatory lung disease. This report describes the design, synthesis and in vitro inhibitory activity of some n