639090-54-3Relevant articles and documents
Tozasertib Analogues as Inhibitors of Necroptotic Cell Death
Hofmans, Sam,Devisscher, Lars,Martens, Sofie,Van Rompaey, Dries,Goossens, Kenneth,Divert, Tatyana,Nerinckx, Wim,Takahashi, Nozomi,De Winter, Hans,Van Der Veken, Pieter,Goossens, Vera,Vandenabeele, Peter,Augustyns, Koen
, p. 1895 - 1920 (2018/03/21)
Receptor interacting protein kinase 1 (RIPK1) plays a crucial role in tumor necrosis factor (TNF)-induced necroptosis, suggesting that this pathway might be druggable. Most inhibitors of RIPK1 are classified as either type II or type III kinase inhibitors. This opened up some interesting perspectives for the discovery of novel inhibitors that target the active site of RIPK1. Tozasertib, a type I pan-aurora kinase (AurK) inhibitor, was found to show a very high affinity for RIPK1. Because tozasertib presents the typical structural elements of a type I kinase inhibitor, the development of structural analogues of tozasertib is a good starting point for identifying novel type I RIPK1 inhibitors. In this paper, we identified interesting inhibitors of mTNF-induced necroptosis with no significant effect on AurK A and B, resulting in no nuclear abnormalities as is the case for tozasertib. Compounds 71 and 72 outperformed tozasertib in an in vivo TNF-induced systemic inflammatory response syndrome (SIRS) mouse model.
As inhibitors of Aurora kinases substituted pyrimidine derivatives
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Paragraph 0326-0330, (2016/10/09)
The present invention relates to a substituted and aurora kinase-inhibiting pyrimidine derivative as represented by formula (I) or (Ia), tautomer, hydrate, solvate, ester or pharmaceutically acceptable salt thereof, and pharmaceutical composition comprising the compounds as active ingredients, as well as uses of the compounds and the pharmaceutical composition thereof in the preparation of drugs for protecting against, treating, curing or alleviating proliferative diseases of a patient.
COMPOUNDS AND METHODS OF USE THEREOF FOR TREATING NEURODEGENERATIVE DISORDERS
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Paragraph 0217; 0218, (2014/07/08)
Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling
Li, Zhengqiu,Hao, Piliang,Li, Lin,Tan, Chelsea Y. J.,Cheng, Xiamin,Chen, Grace Y. J.,Sze, Siu Kwan,Shen, Han-Ming,Yao, Shao Q.
supporting information, p. 8551 - 8556 (2013/09/12)
Less is more: A minimalist "clickable" photo-crosslinker (see scheme) was incorporated with numerous small-molecule kinase inhibitors. The resulting probes were used for both in vitro (cell lysates) and in situ (live cells) proteome profiling, for large-scale identification of their potential cellular kinase targets and shows improved outcomes over previous probes. Copyright
DRUG DISCOVERY METHODS
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Page/Page column 24, (2011/11/12)
The present invention relates to drug discovery methods, particularly methods for assaying compounds for activity as Aurora kinase inhibitors. This invention also relates to a pharmacophore describing compounds that are able to promote a conformational ch
TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS
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Page/Page column 72-73, (2010/12/29)
Compounds of the formula (I) and formula (II) and pharmaceutically acceptable salts thereof.
TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS
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Page/Page column 61, (2010/12/29)
The invention provides Triazine derivatives and further provides methods of using these compounds to modulate protein kinases and for treating diseases and conditions mediated by protein kinases.
AMINOPYRIMIDINES USEFUL AS KINASE INHIBITORS
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Page/Page column 39, (2010/06/16)
The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment
AURORA INHIBITORS CONTAINING A ZINC BINDING MOIETY
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Page/Page column 56, (2009/08/14)
The present invention relates to Aurora inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act as HDAC inhibitors.
KINASE INHIBITORS
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Page/Page column 46, (2010/11/08)
Disclosed are protein kinase inhibitors of Formula Ia and Ib, compositions comprising such inhibitors, and methods of use, thereof. More particularly, these compounds and compositions are inhibitors of Aurora-A (Aurora-2) and Aurora-B (Aurora-1) protein k