Zobrazeno 1 - 10
of 49
pro vyhledávání: '"Chuangxing Guo"'
Autor:
Kephart Susan Elizabeth, Annette John-Baptiste, Deal Judith G, Danlin Gu, Shubha Bagrodia, Cui Jingrong Jean, Shinji Yamazaki, Djamal Bouzida, Pairish Mason Alan, Evan Smith, Chuangxing Guo, Robert Steven Kania, Dong Liming, Angelica Linton, Indrawan James Mcalpine, Cynthia Louise Palmer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:7605-7609
( S )-1-((4-(3-(6-Amino-5-methoxypyridin-3-yl)-1-isopropyl-1 H -pyrazol-4-yl)pyrimidin-2-yl)amino)propan-2-ol, 1 , was recently identified as a potent inhibitor of the oncogenic kinase bRAF. Compounds containing 3-methoxy-2-aminopyridine, as in 1 , c
Autor:
Jon Engebretsen, Martha A. Ornelas, Kephart Susan Elizabeth, Natilie Hosea, Angelica Linton, Asako Nagata, Javier Gonzalez, Samantha Elizabeth Greasley, Chuangxing Guo, Andrea Fanjul, Pairish Mason Alan, Jeff Elleraas
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1230-1236
High throughput cell-based screening led to the identification of 3-aryloxy lactams as potent androgen receptor (AR) antagonists. Refinement of these leads to improve the ADME profile and remove residual agonism led to the discovery of 12, a potent f
Autor:
Qiyue Hu, Kephart Susan Elizabeth, Angelica Linton, Pairish Mason Alan, Ying Jiang, Chuangxing Guo, Ping Kang, Martha A. Ornelas
Publikováno v:
Journal of Medicinal Chemistry. 54:7705-7712
N-{trans-3-[(5-Cyano-6-methylpyridin-2-yl)oxy]-2,2,4,4-tetramethylcyclobutyl}imidazo[1,2-a]pyrimidine-3-carboxamide (1) was recently identified as a full antagonist of the androgen receptor, demonstrating excellent in vivo tumor growth inhibition in
Autor:
Kephart Susan Elizabeth, Angelica Linton, Javier Gonzalez, Kevin D. Bunker, Paul F. Richardson, Chuangxing Guo, Pairish Mason Alan, Martha A. Ornelas, Neal W. Sach
Publikováno v:
Tetrahedron Letters. 52:4760-4763
A new method was developed to synthesize highly functionalized lactams via a one pot reductive amination/lactam formation reaction. This methodology is amenable for parallel synthesis and was used to prepare a large number of lactam analogs in a libr
Publikováno v:
Tetrahedron Letters. 52:1692-1696
Here we report mild, environmentally-friendly reaction conditions which enable the addition–elimination S N Ar reaction between weakly reactive substrates––an aminopyrrolopyrazole template and several substituted pyrimidines. The method was dev
Publikováno v:
Tetrahedron Letters. 51:2909-2913
Here we report an efficient synthesis of sulfamides. 3,5-Lutidine was found to be an optimal solvent and catalyst for the reaction. The method was developed during our efforts to synthesize a series of novel FKBP-12 inhibitors in which the known keto
Autor:
Todd VanArsdale, RoseAnn Ferre, David A. Matthews, Ian Popoff, Marakovits Joseph T, Brion W. Murray, Joseph Piraino, Barbara Mroczkowski, Dong Liming, Stephen Margosiak, Xinjun Hou, M. Catherine Johnson, James Arthur Thomson, Gerrit Los, Eleanor Dagostino, Chuangxing Guo, Samantha Elizabeth Greasley, Hans E. Parge
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5613-5616
Pin1 is a member of the cis-trans peptidyl-prolyl isomerase family with potential anti-cancer therapeutic value. Here we report structure-based de novo design and optimization of novel Pin1 inhibitors. Without a viable lead from internal screenings,
Autor:
Dong Liming, Xinjun Hou, Elizabeth A. Lunney, Corinne E. Augelli-Szafran, Deal Judith G, Christopher F. Bigge, Darin Vanderpool, Raymond Andrew Hudack, Nancy Sue Barta, Bradley William Caprathe, Chuangxing Guo, Steve Bender, Richard E. Showalter, Lorraine Kathleen Fay, Arindam Chatterjee
Publikováno v:
Journal of Medicinal Chemistry. 49:1202-1206
Since the discovery that FK-506 promotes neurite outgrowth, considerable attention has been focused on the development of potent nonimmunosuppressive ligands for FK-506 binding proteins (FKBPs). Such neuroimmunophilin agents have been reported to sho
Autor:
Bo Yang, Ye Sun, Guolan Wei, Youzhi Tong, Chuangliang Xu, Shancheng Ren, Jianguo Hou, Chunyun Chen, Xu Gao, Weidong Xu, Karl Zhou, Ying-Hao Sun, Chuangxing Guo, Tie Zhou
Publikováno v:
Journal of Clinical Oncology. 35:e16511-e16511
e16511 Background: Proxaluatmide is a novel dual MOA androgen receptor (AR) blocker with potent AR antagonist activity and capability to down-regulate AR level. We conducted a first-in-human phase 1 study to investigate safety, tolerability, and phar
Autor:
Li Haitao, Paderes Genevieve Deguzman, Brion W. Murray, Xinjun Hou, RoseAnn Ferre, Marakovits Joseph T, M. Catherine Johnson, Paul S. Humphries, Samantha Elizabeth Greasley, Eugenia Kraynov, Joseph Piraino, Dong Liming, Eleanor Dagostino, Chuangxing Guo
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(17)
The design of potent Pin1 inhibitors has been challenging because its active site specifically recognizes a phospho-protein epitope. The de novo design of phosphate-based Pin1 inhibitors focusing on the phosphate recognition pocket and the successful