834888-63-0Relevant articles and documents
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
TYROSINE KINASE INHIBITORS CONTAINING A ZINC BINDING MOIETY
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Page/Page column 56-57, (2008/06/13)
The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
Discovery of N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays
Lombardo, Louis J.,Lee, Francis Y.,Chen, Ping,Norris, Derek,Barrish, Joel C.,Behnia, Kamelia,Castaneda, Stephen,Cornelius, Lyndon A. M.,Das, Jagabandhu,Doweyko, Arthur M.,Fairchild, Craig,Hunt, John T.,Inigo, Ivan,Johnston, Kathy,Kamath, Amrita,Kan, David,Klei, Herbert,Marathe, Punit,Pang, Suhong,Peterson, Russell,Pitt, Sidney,Schieven, Gary L.,Schmidt, Robert J.,Tokarski, John,Wen, Mei-Li,Wityak, John,Borzilleri, Robert M.
, p. 6658 - 6661 (2007/10/03)
A series of substituted 2-(aminopyridyl)- and 2-(aminopyrimidinyl)thiazole- 5-carboxamides was identified as potent Src/Abl kinase inhibitors with excellent antiproliferative activity against hematological and solid tumor cell lines. Compound 13 was orally active in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels. On the basis of its robust in vivo activity and favorable pharmacokinetic profile, 13 was selected for additional characterization for oncology indications.