Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Wen-Zhen Gu"'
Autor:
Wen-Zhen Gu, Xiao-yue Liang, De-Dong Zhu, Yue-Can Zhang, Ai-Rong Hu, Chuan-Tong Lu, Suwen Jiang, Yao-Ren Hu, Lei Xie
Publikováno v:
Pathology International. 62:565-570
A 15-month boy with fatal hand, foot, and mouth disease (HFMD) exhibited atypical symptoms and progressed rapidly to death. An autopsy was performed the next day and tissue sections were stained for histopathological examination. His intestinal sampl
Autor:
Lisa A. Hasvold, Wen-Zhen Gu, Magdalena Przytulinska, Saul H. Rosenberg, Le Wang, Thomas J. Sowin, Philip Merta, Zehan Chen, Peter Kovar, Chang Park, Haiying Zhang, John Xue, Nan-Horng Lin, Zhan Xiao
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2311-2315
The synthesis and structure-activity relationships (SAR) of Chk1 inhibitors based on a 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one core are described. Specifically, an exploration of the 7 and 8 positions on this previously disclosed core afforded
Autor:
Magdalena Przytulinska, Gaoquan Li, Thomas J. Sowin, Wen-Zhen Gu, Lisa A. Hasvold, Philip Merta, Zhan Xiao, Le Wang, John Xue, Reema Thalji, Kent D. Stewart, Zehan Chen, Zhi-Fu Tao, Nan-Horng Lin, Jennifer J. Bouska, Chang Park, Hexamer Laura, Hing L. Sham, Haiying Zhang, Mai-Ha Bui, Gerard M. Sullivan, Saul H. Rosenberg, Peter Kovar
Publikováno v:
Journal of Medicinal Chemistry. 50:4162-4176
A novel series of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones have been synthesized as potent and selective checkpoint kinase 1 (Chk1) inhibitors via structure-based design. Aided by protein X-ray crystallography, medicinal chemistry efforts led t
Autor:
Hing L. Sham, Russell A. Judge, Akiyo Claiborne, Thomas J. Sowin, Haiying Zhang, Stephen L. Gwaltney, Nan-Horng Lin, Kent D. Stewart, Yunsong Tong, Chang Park, Saul H. Rosenberg, Peter Kovar, Zehan Chen, Wen-Zhen Gu, Robert B. Credo
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:2759-2767
A new class of checkpoint kinase 1 (CHK-1) inhibitors bearing a 1,4-dihydroindeno[1,2-c]pyrazole core was developed after initial hits from high throughput screening. The efficient hit-to-lead process was facilitated by X-ray crystallography and led
Autor:
T. F. Holzman, Uri S. Ladror, Kenneth Jarvis, Hing L. Sham, Mark G. Anderson, Shi-Chung Ng, Le Wang, David Frost, Luis E. Rodriguez, Saul H. Rosenberg, Steven W. Muchmore, John E. Harlan, Jerry Cohen, Debra Ferguson, Yi-Chun Wang, Paul E. Kroeger, Vincent S. Stoll, Gerard M. Sullivan, Ingrid B J K Joseph, Nan-Horng Lin, Wen-Zhen Gu, Haiying Zhang, Clarissa G. Jakob, Kennan C. Marsh, Karl A. Walten
Publikováno v:
Anti-Cancer Drugs. 16:1059-1069
Ras mutation has been detected in approximately 20-30% of all human carcinomas, primarily in pancreatic, colorectal, lung and bladder carcinomas. The indirect inhibition of Ras activity by inhibiting farnesyltransferase (FTase) function is one therap
Autor:
Thomas J. Sowin, Wang Xilu, Steve O’Conner, Lisa A. Hasvold, Wen-Zhen Gu, Hing L. Sham, Jerry Cohen, Gary T. Wang, Robert Gentiles, Haiying Zhang, Charles W. Hutchins, Gerry Sullivan, Weibo Wang, Saul H. Rosenberg
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:153-158
A non-methionine FT inhibitor lead structure ( 1 ) was designed through computer modeling of the peptidomimetic FT inhibitor ABT839. Optimization of this lead resulted in compounds 2e and 2g , with FT IC 50 values of 1.3 and 1.8 nM, GGT IC 50 of 1400
Autor:
Saul H. Rosenberg, Le Wang, Wang Xilu, Jerry Cohen, Hing L. Sham, Nan-Horng Lin, Wen-Zhen Gu, Haiying Zhang, Gary T. Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:5057-5062
Farnesyltransferase inhibitors (FTIs) have emerged as a novel class of anti-cancer agents. Analogs of the potent FTI, 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole, were synthesized and tested in vitro for their inhibitory activities. The most pro
Autor:
Kennan C. Marsh, Jerome Cohen, Nan-Horng Lin, Joy Bauch, Wen-Zhen Gu, Qun Li, Haiying Zhang, Rodger F. Henry, Le Wang, Saul H. Rosenberg, Hing L. Sham
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:4603-4606
Two novel series of potent and selective FTase inhibitors have been synthesized using structure-based design. Medicinal chemistry efforts led to the discovery of compound 4e with potent cellular activity and good oral bioavailability in dog. A synthe
Autor:
Hing L. Sham, Le Wang, Wen-Zhen Gu, Saul A. Rosenberg, Jerry Cohen, Haiying Zhang, Nan-Horng Lin, David Frost
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3821-3825
Farnesyltransferase inhibitors (FTIs) have emerged as a novel class of anticancer agents. Analogues of the potent FTI, 4-[3-biphenyl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile, were synthesized and tested in vitro for thei
Autor:
Hing L. Sham, Lisa A. Hasvold, Jerry Cohen, Weibo Wang, Yunsong Tong, Wen-Zhen Gu, Qun Li, Joy Bauch, Saul H. Rosenberg, Tongmei Li, Nicholas M Leonard, Le Wang, Vincent S. Stoll, Haiying Zhang, Nan-Horng Lin, Kennan C. Marsh
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:1571-1574
A pyridyl moiety was introduced into a previously developed series of farnesyltransferase inhibitors containing imidazole and cyanophenyl (such as 4), resulting in potent inhibitors with improved pharmacokinetics.