796738-71-1Relevant articles and documents
Live-cell imaging and profiling of c-Jun N-terminal kinases using covalent inhibitor-derived probes
Qian, Linghui,Pan, Sijun,Lee, Jun-Seok,Ge, Jingyan,Li, Lin,Yao, Shao Q.
, p. 1092 - 1095 (2019/01/29)
c-Jun N-terminal kinases (JNKs) are involved in critical cellular functions. Herein, small-molecule JNK-targeting probes are reported based on a covalent inhibitor. Together with newly developed two-photon fluorescence Turn-ON reporters and chemoproteomic studies, we showed that some probes may be suitable for live-cell imaging and profiling of JNKs.
Novel imatinib derivatives with altered specificity between Bcr-Abl and FMS, KIT, and PDGF receptors
Skobridis, Konstantinos,Kinigopoulou, Maria,Theodorou, Vassiliki,Giannousi, Emilia,Russell, Alison,Chauhan, Rakhee,Sala, Roberta,Brownlow, Nicola,Kiriakidis, Serafim,Domin, Jan,Tzakos, Andreas G.,Dibb, Nick J.
scheme or table, p. 130 - 139 (2010/11/02)
Imatinib is a clinically important ATP analogue inhibitor that targets the tyrosine kinase domain of the intracellular Abl kinase and the PDGF receptor family. Imatinib has revolutionised the treatment of chronic myeloid leukaemia, which is caused by the oncogene Bcr-Abl and certain solid tumours that harbor oncogenic mutations of the PDGF receptor family. As a leading kinase inhibitor, imatinib also provides an excellent model system to investigate how changes in drug design impact biological activity, which is an important consideration for rational drug design. Herein we report a new series of imatinib derivatives that in general have greater activity against the family of PDGF receptors and poorer activity against Abl, as a result of modifications of the phenyl and N-methylpiperazine rings. These new compounds provide a platform for further drug development against the therapeutically important PDGF receptor family and they also provide insight into the engineering of drugs with altered biological activity.
N-PHENYL-2-PYRIMIDINE-AMINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
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Page 26, (2010/02/09)
The present invention relates to an N-phenyl-2-pyrimidine-amine derivative showing a superior effect on tumor, lung cancer, gastric cancer, etc. of warm-blooded animals and its salt. The present invention also relates to a process for preparing the compound and a pharmaceutical composition for the prevention and treatment of such diseases as tumor, lung cancer, gastric cancer, etc., which comprises the compound as an active ingredient.