Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Yunsong Tong"'
Autor:
Andrew J. Souers, Wei Qiu, Thomas D. Penning, Darren C. Phillips, Xiaoqin Liu, Rick F. Clark, Joel D. Leverson, Amanda M. Olson, Chunqiu Lai, Daniel H. Albert, Gui-Dong Zhu, Yunsong Tong, Peter Kovar, Kenton L. Longenecker, Anthony Mastracchio, Morey L. Smith, Bailin Shaw, Alan S. Florjancic, Stephen K. Tahir, Donald J. Osterling
Publikováno v:
ACS Med Chem Lett
[Image: see text] Cyclin-dependent kinase 9 (CDK9) is a serine/threonine kinase involved in the regulation of transcription elongation. An inhibition of CDK9 downregulates a number of short-lived proteins responsible for tumor maintenance and surviva
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d85e60b25f3e832de4e347a9da8d597e
https://doi.org/10.1021/acsmedchemlett.1c00161
https://doi.org/10.1021/acsmedchemlett.1c00161
Autor:
Philip J. Merta, Amanda M. Olson, Fritz G. Buchanan, Nirupama B. Soni, Donald J. Osterling, Alan S. Florjancic, Debra Ferguson, David Maag, Eric F. Johnson, Yunsong Tong, Alexander R. Shoemaker, Maricel Torrent, Kenneth D. Bromberg, Thomas D. Penning, Loren M. Lasko
Publikováno v:
ACS Medicinal Chemistry Letters. 6:58-62
Aided by molecular modeling, compounds with a pyrimidine-based tricyclic scaffold were designed and confirmed to inhibit Wee1 kinase. Structure-activity studies identified key pharmacophores at the aminoaryl and halo-benzene regions responsible for b
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0b451c835e91d1f244b2b91708eb295
https://doi.org/10.1021/ml5002745
https://doi.org/10.1021/ml5002745
Autor:
Kerren K. Swinger, Magdalena Przytulinska, Yunsong Tong, Alan S. Florjancic, Eric F. Johnson, Philip J. Merta, Kent D. Stewart, Thomas D. Penning, Nirupama B. Soni, Alexander R. Shoemaker, John E. Harlan, Haizhong Zhu
Publikováno v:
ACS Medicinal Chemistry Letters. 4:211-215
To investigate the role played by the unique pre-DFG residue Val 195 of Cdc7 kinase on the potency of azaindole-chloropyridines (1), a series of novel analogues with various chloro replacements were synthesized and evaluated for their inhibitory acti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d0d5106adb466152cb74c85ee58f5d7b
https://doi.org/10.1021/ml300348c
https://doi.org/10.1021/ml300348c
Autor:
Niru B. Soni, Eric F. Johnson, Joel D. Leverson, Thomas D. Penning, Keith W. Woods, Yan Shi, Loren M. Lasko, Julie M. Miyashiro, Alan S. Florjancic, E. K.-H. Han, Chunqiu Lai, Alexander R. Shoemaker, Yunsong Tong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1940-1943
We have investigated the SAR of a series of pyrimidinone-containing Cdc7 kinase inhibitors. A wide range of amine substitutions give potent compounds with activities (K(i)) less than 1nM. Kinase selectivity is reasonable and cytotoxicity corresponds
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bdf3f74c76d9ced20f6761e60f152a42
https://doi.org/10.1016/j.bmcl.2012.01.041
https://doi.org/10.1016/j.bmcl.2012.01.041
Autor:
Xuesong Liu, Vincent L. Giranda, Luis E. Rodriguez, Paul A. Ellis, Donald J. Osterling, Magdalena Przytulinska, David Frost, Thomas D. Penning, Jason Stavropoulos, Cherrie K. Donawho, Yunsong Tong, Eric F. Johnson, Joel D. Leverson, Jennifer J. Bouska, Yan Shi, Patrick A. Marcotte, Amanda M. Olson, Sheela A. Thomas, Nirupama B. Soni, Yan Luo
Publikováno v:
Journal of Medicinal Chemistry. 52:6803-6813
Small molecule inhibitors of PARP-1 have been pursued by various organizations as potential therapeutic agents either capable of sensitizing cytotoxic treatments or acting as stand-alone agents to combat cancer. As one of the strategies to expand our
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::adaa42993a9837a478796b4a1a429391
https://doi.org/10.1021/jm900697r
https://doi.org/10.1021/jm900697r
Autor:
Nan-Horng Lin, Zhi-Fu Tao, Philip Merta, Thomas J. Sowin, Zehan Chen, Yunsong Tong, Magdalena Przytulinska, Haiying Zhang, Saul H. Rosenberg, Peter Kovar, Gaoquan Li
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:6499-6504
A variety of macrocyclic urea compounds were prepared as potent Chk1 inhibitors by modifying the C5 position of the benzene ring of the macrocyclic urea with ether moieties, aliphatic carbon chains, amide and halides. Enzymatic activity less than 20
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afe89467cf731d7d70b5b8e757707311
https://doi.org/10.1016/j.bmcl.2007.09.088
https://doi.org/10.1016/j.bmcl.2007.09.088
Autor:
Zhi-Fu Tao, Nan-Horng Lin, Hing L. Sham, Saul H. Rosenberg, Yunsong Tong, Kent D. Stewart, Peter Kovar, Mai-Ha Bui, Zehan Chen, Haiying Zhang, Philip J. Merta, Chang Park, Akiyo Claiborne, Magdalena Przytulinska, Donald J. Osterling, Thomas J. Sowin, Gaoquan Li, Jennifer J. Bouska, Amanda Olson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5665-5670
A series of 1,4-dihydroindeno[1,2-c]pyrazole compounds with a cyanopyridine moiety at the 3-position of the tricyclic pyrazole core was explored as potent CHK-1 inhibitors. The impact of substitutions at the 6 and/or 7-position of the core on pharmac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c39031465133b26ad586da1c75f4902
https://doi.org/10.1016/j.bmcl.2007.07.069
https://doi.org/10.1016/j.bmcl.2007.07.069
Autor:
Tim J. Stratton, Yunsong Tong, Jian Wu, Hing L. Sham, Nan-Horng Lin, Elizabeth A. Everitt, Bernard P. Murry, Kent D. Stewart, Zehan Chen, Haiying Zhang, Robert B. Credo, Saul H. Rosenberg, Philip Merta, Zhi-Fu Tao, Peter Kovar, Jennifer J. Bouska, Thomas J. Sowin, Dean Hickman, Akiyo Claiborne, Ran Guan, Magdalena Pyzytulinska
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3618-3623
A study on substitutions at the four open positions on the phenyl ring of the 1,4-dihydroindeno[1,2-c]pyrazoles as potent CHK-1 inhibitors is described. Bis-substitution at both the 6- and 7-positions led to inhibitors with IC(50) values below 0.3nM.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cc87418630f9ea950ee9d845b7228ffb
https://doi.org/10.1016/j.bmcl.2007.04.055
https://doi.org/10.1016/j.bmcl.2007.04.055
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ae47e5b591d4943cf0905bb26642807
https://doi.org/10.1016/j.bmc.2007.01.012
https://doi.org/10.1016/j.bmc.2007.01.012
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.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7965ad3aa6778f724633dd2bec484095
https://doi.org/10.1016/s0960-894x(03)00195-1
https://doi.org/10.1016/s0960-894x(03)00195-1