179411-72-4Relevant academic research and scientific papers
A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFRL858R/T790Mmutant with improved pharmacokinetic properties
Yu, Lei,Huang, Minhao,Xu, Tianfeng,Tong, Linjiang,Yan, Xiao-e,Zhang, Zhang,Xu, Yong,Yun, Caihong,Xie, Hua,Ding, Ke,Lu, Xiaoyun
supporting information, p. 1107 - 1117 (2016/12/30)
Structural optimization of pyrido[2,3-d]pyrimidin-7-ones was conducted to yield a series of new selective EGFRT790Minhibitors with improved pharmacokinetic properties. One of the most promising compound 9s potently suppressed EGFRL858R/T790Mkinase and inhibited the proliferation of H1975?cells with IC50values of 2.0?nM and 40?nM, respectively. The compound dose-dependently induced reduction of the phosphorylation of EGFR and downstream activation of ERK in NCI[sbnd]H1975?cells. It also exhibited moderate plasma exposure after oral administration and an oral bioavailability value of 16%. Compound 9s may serve as a promising lead compound for further drug discovery overcoming the acquired resistance of non-small cell lung cancer (NSCLC) patients.
AZIDOPHENYLCYANOGUANIDINES AS PHOTOAFFINITY PROBES
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, (2008/06/13)
This invention comprises novel compounds that are useful and effective as photoaffinity probes useful for the identification of the biochemical components that form K ATP channels in smooth muscle cells. The probes are described by the formula below, STR1 where R. sub.1 is H, C. sub.1-3 alkyl; R 2 is H, C 1-3 alkyl; or R 1 and R 2 may be joined together to form C 3-6 cycloalkyl, or C 3-6 cycloalkyl optionally substituted with C 1-4 alkyl;R 3 is C 1-6 alkyl, or C 6-12 aryl optionally substituted with 1-3 Halogens; or suitable salts thereof.
