71478-56-3Relevant academic research and scientific papers
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases
Baska, Ferenc,Sipos, Anna,?rfi, Zoltán,Nemes, Zoltán,Dobos, Judit,Szántai-Kis, Csaba,Szabó, Eszter,Szénási, Gábor,Dézsi, László,Hamar, Péter,Cserepes, Mihály T.,Tóvári, József,Garamv?lgyi, Rita,Krekó, Marcell,?rfi, László
supporting information, (2019/10/16)
Aberrant activation of FMS-like tyrosine receptor kinase 3 (FLT3) is implicated in the pathogenesis of acute myeloid leukemia (AML) in 20–30% of patients. In this study we identified a highly selective (phenylethenyl)quinazoline compound family as novel potent inhibitors of the FLT3-ITD and FLT3-D835Y kinases. Their prominent effects were confirmed by biochemical and cellular proliferation assays followed by mice xenograft studies. Our modelling experiments and the chemical structures of the compounds predict the possibility of covalent inhibition. The most effective compounds triggered apoptosis in FLT3-ITD AML cells but had either weak or no effect in FLT3-independent leukemic and non-leukemic cell lines. Our results strongly suggest that our compounds may become therapeutics in relapsing and refractory AML disease harboring various ITD and tyrosine kinase domain mutations, by their ability to overcome drug resistance.
SUBSTITUTED PYRROLO[1,2-α]TRIAZINES AND RELATED COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
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Paragraph 00181, (2017/12/14)
The invention provides substituted pyrrolo[1,2-α]triazine compounds, related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinso
Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors
Liu, Kevin K.C.,Huang, Xiaojun,Bagrodia, Shubha,Chen, Jeffrey H.,Greasley, Samantha,Cheng, Hengmiao,Sun, Shaoxian,Knighton, Dan,Rodgers, Caroline,Rafidi, Kristina,Zou, Aihua,Xiao, Jiezhan,Yan, Shengyong
scheme or table, p. 1270 - 1274 (2011/04/16)
Intra-molecular hydrogen bonding was introduced to the quinazoline motif to form a pseudo ring (intra-molecular H-bond scaffold, iMHBS) to mimic our previous published core structures, pyrido[2.3-D]pyrimidin-7-one and pteridinone, as PI3K/mTOR dual inhibitors. This design results in potent PI3K/mTOR dual inhibitors and the purposed intra-molecular hydrogen bonding structure is well supported by co-crystal structure in PI3Kγ enzyme. In addition, a novel synthetic route was developed for these analogs.
Quinoline and quinazoline derivatives having corticotropin releasing factor (CRF) antagonist activity
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Page column 10, (2010/02/05)
The present invention relates to novel compounds, to a method for the preparation of these novel compounds, to pharmaceutical compositions containing one or more of these compounds as an active component and to methods of using these in the treatment of s
Search for non-steroidal anti-inflammatory agents. Part 1: Synthesis of 2-alkyl/aryl-3-benzimidazolylalkylquinazolon-4(3H)-ones.
Tiwari,Zaidi,Satsangi
, p. 73 - 75 (2007/10/02)
Sixteen title compounds have been synthesized and some of them have shown interesting results in antiinflammatory screening against carrageenin-induced inflammation. In addition, the compounds were found to be central nervous system depressants and relatively non-toxic.
