175135-74-7Relevant articles and documents
Indole derivative and medical application thereof
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Paragraph 0121-0125, (2020/12/15)
The invention discloses an indole compound with FABP4/5 inhibitory activity and a preparation method and medical application of the indole compound. The indole compound is a compound of which the structural formula is shown as a formula I, and pharmaceutically acceptable salt or ester or solvate of the compound. The compound shown in the formula I is a novel FABP4/5 inhibitor and can be used for preparing medicines for preventing or treating FABP4/5 related diseases.
Design, synthesis and pharmacological evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents
Zhou, Shunguang,Ren, Jianguo,Liu, Mingmei,Ren, Lixiang,Liu, Yajing,Gong, Ping
, p. 30 - 42 (2014/12/11)
Two series of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 2,4-imidazolinedione/pyrazolone scaffold were designed, synthesized and evaluated for their c-Met kinase inhibition and cytotoxicity against HT-29, H460, A549, MKN-45, and U87MG cancer cell lines in vitro. The pharmacological data indicated that most of the tested compounds showed moderate to significant cytotoxicity and high selectivity against HT-29, H460 and A549 cancer cell lines as compared with foretinib. The SAR analyses indicated that compounds with halogen groups, especially trifluoromethyl groups at 2-position on the phenyl ring (moiety B) were more effective. In this study, a promising compound 17 (c-Met IC50= 2.20 nM, a multi-target tyrosine kinase inhibitor) showed the most potent antitumor activities with IC50values of 0.14 μM, 0.18 μM, 0.09 μM, 0.03 μM, and 1.06 μM against HT-29, H460, A549, MKN-45, and U87MG cell lines, respectively.