Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Martin W. Rowbottom"'
Autor:
Mark W. Holladay, Shripad S. Bhagwat, Michael Williams, Bruce D. Dorsey, Raffaella Faraoni, Julius L. Apuy, Mark A. Ator, Darren E. Insko, Mehran Yazdanian, Dana Gitnick, Mangeng Cheng, Ronald R. Nepomuceno, Kathryn Hunter, Merryl D. Cramer, Hugh Zhao, Michael F. Gardner, Pawel Dobrzanski, Ruwanthi N. Gunawardane, Susan Jones-Bolin, Martin W. Rowbottom, Robert C. Armstrong, Bruce Ruggeri, Joyce James
PDF file - 74K, CEP-32496 Supplemental Data.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e595ddea4dcb7e0d0c551afc2da871ae
https://doi.org/10.1158/1535-7163.22498993.v1
https://doi.org/10.1158/1535-7163.22498993.v1
Autor:
Andiliy G. Lai, Katherine Nguyen, Gretchen Bain, Lance Goulet, Imelda Calderon, Fei Huang, Deidre A. MacKenna, Kristen E. Shannon, Janice Darlington, Patricia Prodanovich, John H. Hutchinson, David Lonergan, Angelina M. Santini, Gina L. Ma, Jilly F. Evans, Taylor Lasof, Martin W. Rowbottom, Christopher D. King
Publikováno v:
Journal of Medicinal Chemistry. 60:4403-4423
LOXL2 catalyzes the oxidative deamination of ε-amines of lysine and hydroxylysine residues within collagen and elastin, generating reactive aldehydes (allysine). Condensation with other allysines or lysines drives the formation of inter- and intramo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2036ae21d4c3a736f5b1814c4ba1e04
https://doi.org/10.1021/acs.jmedchem.7b00345
https://doi.org/10.1021/acs.jmedchem.7b00345
Autor:
Gretchen Bain, David Lonergan, Jilly F. Evans, Christopher D. King, Martin W. Rowbottom, John H. Hutchinson, Pat Prodanovich, Janice Darlington
Publikováno v:
ACS medicinal chemistry letters. 8(4)
Two series of novel LOXL2 enzyme inhibitors are described: benzylamines substituted with electron withdrawing groups at the para-position and 2-substituted pyridine-4-ylmethanamines. The most potent compound, (2-chloropyridin-4-yl)methanamine 20 (hLO
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56a71d6663f4f9b872f646bf2fcb6880
https://pubmed.ncbi.nlm.nih.gov/28435530
https://pubmed.ncbi.nlm.nih.gov/28435530
Autor:
Warren Wade, Martin W. Rowbottom, Yongsheng Chen, R. Scott Struthers, Haig Bozigian, Qiu Xie, Takung Chen, Fabio C. Tucci, Jenny Wen, Dongpei Wu, Charles Q. Huang, Joseph Pontillo, Zhiqiang Guo, John Saunders, Yun-Fei Zhu, Ajay Madan, Chen Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3301-3305
Incorporation of a carboxylic acid into a series of uracil derivatives as hGnRH-R antagonists resulted in a significant reduction of CYP3A4 inhibitory activity. Highly potent hGnRH antagonists with low CYP3A4 inhibitory liability, such as 8a and 8d,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f87415e860f1d269dfd364ccadd72136
https://doi.org/10.1016/j.bmcl.2008.04.036
https://doi.org/10.1016/j.bmcl.2008.04.036
Autor:
Jason Haelewyn, Brian Dyck, Troy Vickers, Junko Tamiya, Mingzhu Zhang, Linh Nguyen, Martin W. Rowbottom, David A. Schwarz, Val S. Goodfellow, Monica S. Mistry, Christopher E. Heise, Jonathan Grey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2535-2539
A series of thienopyrimidinone bis-aminopyrrolidine ureas were designed, synthesized, and evaluated for their ability to bind melanin-concentrating hormone receptor-1. These compounds exhibit potent binding affinity (K(i)=3 nM) and good in vitro meta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe96e12383f0fb984ce0e4f668bb4640
https://doi.org/10.1016/j.bmcl.2007.02.012
https://doi.org/10.1016/j.bmcl.2007.02.012
Autor:
Fabio C. Tucci, Martin W. Rowbottom, Susan K. Sullivan, R. Scott Struthers, Yang Sai, Collin F. Regan, Shelby Reijmers, Chen Chen, Zhiqiang Guo, Qiu Xie, Dongpei Wu, Yun-Fei Zhu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3685-3690
SAR studies of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists resulted in potent compounds. The best compound from the series had a binding affinity of 2 nM.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b37e6872c5e7cde2a7d2bace282ab30
https://doi.org/10.1016/j.bmcl.2005.05.038
https://doi.org/10.1016/j.bmcl.2005.05.038
Autor:
Martin W. Rowbottom, Mingzhu Zhang, Christopher E. Heise, Brian Dyck, Liren Zhao, Val S. Goodfellow, John Saunders, Junko Tamiya, Jonathan Grey, David A. Schwarz, Troy Vickers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:999-1004
Ureas derived from two substituted 3-aminopyrrolidine subunits were prepared as constrained analogs of a linear lead compound and tested as antagonists of the MCH1 receptor. The series was optimized for substitution and stereochemistry to generate a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::368afcbd91cbc5e0e9a3a44839ca5604
https://doi.org/10.1016/j.bmcl.2004.12.036
https://doi.org/10.1016/j.bmcl.2004.12.036
Autor:
Xin-Jun Liu, Yinghong Gao, Zhiqiang Guo, Martin W. Rowbottom, Timothy D. Gross, Anne L Killam Bonneville, Acevedo O, Caroline W. Chen, Struthers Rs, Haig Bozigian, Greg J. Reinhart, Ta-Kung Chen, Fabio C. Tucci, Nicholas Ling, John Saunders, Qui Xie, Yun-Fei Zhu
Publikováno v:
Journal of Medicinal Chemistry. 48:1169-1178
Further structure-activity relationship studies of a series of substituted uracils at the 1, 3, and 5 positions resulted in the discovery of several potent antagonists of the human gonadotropin-releasing hormone receptor. Uracils bearing a side chain
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87529259eebd56ca0c42b5b5375da127
https://doi.org/10.1021/jm049218c
https://doi.org/10.1021/jm049218c
Autor:
Lee Carter, Oscar Acevedo, Susan K. Sullivan, Yun-Fei Zhu, Patrick J. Connors, John Saunders, Qiu Xie, Andrew Fisher, Chen Chen, Zhiqiang Guo, R. Scott Struthers, Manisha Moorjani, Martin W. Rowbottom, Fabio C. Tucci, Timothy D. Gross
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:4967-4973
The synthesis of a series of ( R )-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5 is described. SAR around C-5 of the uracil led to the discovery that a 2-thienyl or (2-phenyl)thi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afab3c785ff0457b782440bfeb65d930
https://doi.org/10.1016/j.bmcl.2004.07.022
https://doi.org/10.1016/j.bmcl.2004.07.022
Autor:
Patrick J. Connors, Liping Jin, Haig Bozigian, Timothy D. Gross, Fabio C. Tucci, Ta Kung Chen, R. Scott Struthers, Chen Chen, Greg J. Reinhart, John Saunders, Qiu Xie, Martin W. Rowbottom, Yinghong Gao, Zhiqiang Guo, Anne L Killam Bonneville, Andrew Fisher, Yun-Fei Zhu
Publikováno v:
Journal of Medicinal Chemistry. 47:3483-3486
Uracils possessing N-3 side chains derived from various amino alcohols were designed and synthesized as potent human gonadotropin releasing hormone receptor antagonists. The compounds herein presented displayed superior metabolic stability than their
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05a763114ebf99451c3177008485abea
https://doi.org/10.1021/jm049791w
https://doi.org/10.1021/jm049791w