Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Sze-Wan Li"'
Autor:
David Cescon, Jeffrey Bruce, Lisa-Maria Yonemoto, Philippe L. Bedard, Trisha Denny, Dennis J. Slamon, Mark R. Bray, Tak W. Mak, Zev A. Wainberg, Sze-Wan Li, Graham C. Fletcher, Peter Brent Sampson, Zachary William Neil Veitch, Trevor J. Pugh, Richard Brokx
Publikováno v:
British Journal of Cancer
British journal of cancer, vol 121, iss 4
British journal of cancer, vol 121, iss 4
Background CFI-400945 is a first-in-class oral inhibitor of polo-like kinase 4 (PLK4) that regulates centriole duplication. Primary objectives of this first-in-human phase 1 trial were to establish the safety and tolerability of CFI-400945 in patient
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
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
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
Publikováno v:
Tetrahedron Letters. 56:3137-3140
The intramolecular Schmidt reaction of ketones and tethered azides is an efficient method for the generation of amides and lactams. This reaction is catalyzed by Lewis acids, which tightly bind the strongly basic amide product and result in product i
Autor:
Fuqiang Ban, Dan Chi-Chia Lin, Erin Green, Sze-Wan Li, Guohua J. Pan, Richard J. Hodgson, Miklos Feher, Yong Liu, Wei Qiu, Olga Plotnikova, Narendra Kumar B. Patel, Grace Ng, Marees Harris-Brandts, Guodong Mao, Nickolay Y. Chirgadze, Don E. Awrey, Irina Beletskaya, Henry W. Pauls, Yunhui Lang, Ping Huang, Vincent Nadeem, Xin Wei, Tak W. Mak, Genie Leung, Reza Kiarash, Jacqueline M. Mason, Louise Edwards, Radoslaw Laufer, Xunyi Luo
Publikováno v:
Bioorganic & Medicinal Chemistry. 22:4968-4997
TTK kinase was identified by in-house siRNA screen and pursued as a tractable, novel target for cancer treatment. A screening campaign and systematic optimization, supported by computer modeling led to an indazole core with key sulfamoylphenyl and ac
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
Publikováno v:
Journal of the American Chemical Society. 135:9000-9009
A method for carrying out the intramolecular Schmidt reaction of alkyl azides and ketones using a substoichiometric amount of catalyst is reported. Following extensive screening, the use of the strong hydrogen-bond-donating solvent hexafluoro-2-propa
Publikováno v:
Organic Letters. 12:1244-1247
The tricyclic core of the cylindricine or lepadiformine families of alkaloid natural products was assembled via a Prins addition/intramolecular Schmidt rearrangement under Lewis acid conditions. Both single-pot and two-stage variations of this proces
Publikováno v:
ChemInform. 46
Starting from azide-tethered ketones the title reaction is applied to the preparation of amides and lactams.