Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Donald E. Awrey"'
Autor:
Henry W. Pauls, Peter Brent Sampson, Guodong Mao, Irina Beletskaya, Guohua Pan, Tak W. Mak, Yong Liu, Bryan T. Forrest, Sze-Wan Li, Narendra Kumar B. Patel, Xin Wei, Miklos Feher, Richard J. Hodgson, Jacqueline M. Mason, Erin Green, Reza Kiarash, Louise Edwards, Radoslaw Laufer, Xunyi Luo, Fuqiang Ban, Donald E. Awrey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:4625-4630
Previous efforts from our laboratory demonstrated that (E)-3-((3-(E)-vinylaryl)-1H-indazol-6-yl)methylene)-indolin-2-ones are potent PLK4 inhibitors with in vivo anticancer efficacy upon IP dosing. As part of a continued effort to develop selective a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::79d1a79d7de4b3d68ced13620c054ca4
https://doi.org/10.1016/j.bmcl.2016.08.063
https://doi.org/10.1016/j.bmcl.2016.08.063
Autor:
Tak W. Mak, Xin Wei, Guodong Mao, Grace Ng, Richard Brokx, Dan Chi-Chia Lin, Graham C. Fletcher, Miklos Feher, Olga Plotnikova, Richard J. Hodgson, Radoslaw Laufer, Henry W. Pauls, Jacqueline M. Mason, Yunhui Lang, Brian Madeira, Irina Beletskaya, Sze-Wan Li, Yong Liu, Yi Che, Donald E. Awrey, Reza Kiarash, Mark R. Bray
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:3562-3566
TTK/Mps1 is a key kinase controlling progression of cell division via participation in the mitotic spindle assembly checkpoint and is overexpressed in a number of human cancers. Herein we report the discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba09af33425cf05a065bc4b1c08a55bc
https://doi.org/10.1016/j.bmcl.2016.06.021
https://doi.org/10.1016/j.bmcl.2016.06.021
Autor:
Mark R. Bray, Wei Qiu, Radoslaw Laufer, Olga Plotnikova, Henry W. Pauls, Richard Brokx, Dan Chi-Chia Lin, Graham C. Fletcher, Richard J. Hodgson, Sze-Wan Li, Narendra Kumar B. Patel, Peter Brent Sampson, Jacqueline M. Mason, Irina Beletskaya, Yunhui Lang, Xin Wei, Yi Che, Reza Kiarash, Tak W. Mak, Miklos Feher, Grace Ng, Donald E. Awrey, Yong Liu, Nickolay Y. Chirgadze
Publikováno v:
ACS Medicinal Chemistry Letters. 7:671-675
This work describes a scaffold hopping exercise that begins with known imidazo[1,2-a]pyrazines, briefly explores pyrazolo[1,5-a][1,3,5]triazines, and ultimately yields pyrazolo[1,5-a]pyrimidines as a novel class of potent TTK inhibitors. An X-ray str
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b3996eda3d4b7410ff16b6aa6d5433d5
https://doi.org/10.1021/acsmedchemlett.5b00485
https://doi.org/10.1021/acsmedchemlett.5b00485
Autor:
Peter B. Sampson, Yong Liu, Bryan Forrest, Graham Cumming, Sze-Wan Li, Narendra Kumar Patel, Louise Edwards, Radoslaw Laufer, Miklos Feher, Fuqiang Ban, Donald E. Awrey, Guodong Mao, Olga Plotnikova, Richard Hodgson, Irina Beletskaya, Jacqueline M. Mason, Xunyi Luo, Vincent Nadeem, Xin Wei, Reza Kiarash, Brian Madeira, Ping Huang, Tak W. Mak, Guohua Pan, Henry W. Pauls
Publikováno v:
Journal of Medicinal Chemistry. 58:147-169
Previous publications from our laboratory have introduced novel inhibitors of Polo-like kinase 4 (PLK4), a mitotic kinase identified as a potential target for cancer therapy. The search for potent and selective PLK4 inhibitors yielded (E)-3-((1H-inda
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::09a88499af90e226793ff88203ec36fb
https://doi.org/10.1021/jm5005336
https://doi.org/10.1021/jm5005336
Autor:
Nachum Kaplan, Judd Berman, Elias Bardouniotis, Jeremy Yethon, Barry Hafkin, Donald E. Awrey, Pauls Henry W
Publikováno v:
Journal of Chemotherapy (Florence, Italy)
AFN-1252 is a novel inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 exhibits typical MIC(90) values of ≤0·015 μg/ml against diverse clinical isolates of S. aureus, oral absorption, long eliminatio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d5889345e61026271de1bbf717c7c5a9
https://doi.org/10.1179/1973947812y.0000000063
https://doi.org/10.1179/1973947812y.0000000063
Autor:
Elias Bardouniotis, Nachum Kaplan, Molly B. Schmid, Judd Berman, Donald E. Awrey, Rosanne Thalakada, Mandy Dorsey, Barry Hafkin, Monique Albert, Teresa E. Clarke, Jeremy Yethon, Vladimir Romanov, Pauls Henry W, Jaillal Ramnauth
Publikováno v:
Antimicrobial Agents and Chemotherapy. 56:5865-5874
The mechanism of action of AFN-1252, a selective inhibitor of Staphylococcus aureus enoyl-acyl carrier protein reductase (FabI), which is involved in fatty acid biosynthesis, was confirmed by using biochemistry, macromolecular synthesis, genetics, an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e1234a5b194110a296575384bd9fe6c
https://doi.org/10.1128/aac.01411-12
https://doi.org/10.1128/aac.01411-12
Autor:
Nachum Kaplan, Vladimir Romanov, Pauls Henry W, Elias Bardouniotis, Teresa E. McGrath, Christine Picard, Dhushy Thambipillai, Andrew Leeson, Donald E. Awrey, Judd Berman, Peter Brent Sampson, Sean Handerson, Megan Domagala
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5355-5358
Spiropiperidine naphthyridinone inhibitors of Staphylococcus aureus and Escherichia coli FabI have been prepared. Compounds 14a and 14c were identified as having sub-nanomolar E. coli FabI activity and are among the most potent FabI inhibitors yet de
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::029551bc2bb4366b841dacecb1817ae3
https://doi.org/10.1016/j.bmcl.2009.07.129
https://doi.org/10.1016/j.bmcl.2009.07.129
Autor:
Yunhui Lang, Louise Edwards, Radoslaw Laufer, Yi Che, Dan Chi-Chia Lin, Yong Liu, Bryan T. Forrest, Sze-Wan Li, Mark R. Bray, Tak W. Mak, Narendra Kumar B. Patel, Xin Wei, Henry W. Pauls, Nickolay Y. Chirgadze, Reza Kiarash, Wei Qiu, Olga Plotnikova, Brian Madeira, Graham C. Fletcher, Richard J. Hodgson, Fuqiang Ban, Miklos Feher, Guodong Mao, Grace Ng, Irina Beletskaya, Donald E. Awrey, Jacqueline M. Mason, Peter Brent Sampson
Publikováno v:
Journal of medicinal chemistry. 58(8)
The acetamido and carboxamido substituted 3-(1H-indazol-3-yl)benzenesulfonamides are potent TTK inhibitors. However, they display modest ability to attenuate cancer cell growth; their physicochemical properties, and attendant pharmacokinetic paramete
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a417f7f080d3add29660da28a0bca0d4
https://pubmed.ncbi.nlm.nih.gov/25763473
https://pubmed.ncbi.nlm.nih.gov/25763473
Autor:
Peter B, Sampson, Yong, Liu, Bryan, Forrest, Graham, Cumming, Sze-Wan, Li, Narendra Kumar, Patel, Louise, Edwards, Radoslaw, Laufer, Miklos, Feher, Fuqiang, Ban, Donald E, Awrey, Guodong, Mao, Olga, Plotnikova, Richard, Hodgson, Irina, Beletskaya, Jacqueline M, Mason, Xunyi, Luo, Vincent, Nadeem, Xin, Wei, Reza, Kiarash, Brian, Madeira, Ping, Huang, Tak W, Mak, Guohua, Pan, Henry W, Pauls
Publikováno v:
Journal of medicinal chemistry. 58(1)
Previous publications from our laboratory have introduced novel inhibitors of Polo-like kinase 4 (PLK4), a mitotic kinase identified as a potential target for cancer therapy. The search for potent and selective PLK4 inhibitors yielded (E)-3-((1Hindaz
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::160efe8c1bbad6cc1acf1625e82022f2
https://pubmed.ncbi.nlm.nih.gov/25723005
https://pubmed.ncbi.nlm.nih.gov/25723005
Autor:
Peter B. Sampson, Yong Liu, Narendra Kumar Patel, Miklos Feher, Bryan Forrest, Sze-Wan Li, Louise Edwards, Radoslaw Laufer, Yunhui Lang, Fuqiang Ban, Donald E. Awrey, Guodong Mao, Olga Plotnikova, Genie Leung, Richard Hodgson, Jacqueline Mason, Xin Wei, Reza Kiarash, Erin Green, Wei Qiu, Nickolay Y. Chirgadze, Tak W. Mak, Guohua Pan, Henry W. Pauls
Publikováno v:
Journal of medicinal chemistry. 58(1)
Polo-like kinase 4 (PLK4), a unique member of the polo-like kinase family of serine-threonine kinases, is a master regulator of centriole duplication that is important for maintaining genome integrity. Overexpression of PLK4 is found in several human
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1db45474216f629dfe05ee2b429ad8b7
https://pubmed.ncbi.nlm.nih.gov/24867403
https://pubmed.ncbi.nlm.nih.gov/24867403