15018-50-5Relevant articles and documents
Selective cell adhesion inhibitors: Barbituric acid based α4β7-MAdCAM inhibitors
Harriman, Geraldine C.,Brewer, Matthias,Bennett, Robert,Kuhn, Cyrille,Bazin, Marc,Larosa, Greg,Skerker, Paul,Cochran, Nancy,Gallant, Debra,Baxter, Deborah,Picarella, Dominic,Jaffee, Bruce,Luly, Jay R.,Briskin, Michael J.
, p. 2509 - 2512 (2008)
A novel series of barbituric acid derivatives were identified as selective inhibitors of α4β7 MAdCAM (mucosal addressin cell adhesion molecule-1) interactions via a high throughput screening exercise. These inhibitors were optimized to submicromolar potencies in whole cell adhesion assays, retaining their selectivity over α4β1 VCAM.
Pyrimidones including six hydrogens quinoline compound and its preparation method and application
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Paragraph 0178; 0179, (2018/02/04)
The invention relates to a quinolines compound containing hexahydropyrimidone, which is represented by a formula I, as well as pharmaceutically acceptable configurational isomers, salts, hydrates, solvates and prodrugs thereof. According to the quinolines compound, substituent groups R1, R2, R3, X, Y, Z and n have definitions given in the specification. The invention further relates to the compound of the formula I and the configurational isomers which have a very strong effect of inhibiting c-Met kinase, further relates to an application of the compounds and the pharmaceutically acceptable salts, hydrates, solvates or prodrugs in preparing a medicine for treating diseases caused by hydrates high expression of the c-Met kinase, and particularly relates to an application of a medicine for preparing a medicine for treating and/or preventing cancers.
Discovery of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 5-(aminomethylene)pyrimidine-2,4,6-trione moiety as c-Met kinase inhibitors
Tang, Qidong,Zhang, Guogang,Du, Xinming,Zhu, Wufu,Li, Ruijuan,Lin, Huafang,Li, Pengcheng,Cheng, Maosheng,Gong, Ping,Zhao, Yanfang
, p. 1236 - 1249 (2014/03/21)
A series of novel quinoline derivatives bearing 5-(aminomethylene) pyrimidine-2,4,6-trione moiety were designed, synthesized, and evaluated for their c-Met kinase inhibitory activities and antiproliferative activities against 5 cancer cell lines (HT-29, H460, MKN-45, A549, and U87MG) in vitro. Most compounds showed moderate to excellent potency, with the most promising analogue 45 (c-Met half-maximal inhibitory concentration [IC50] = 1.15 nM) showing high selectivity versus 5 other tyrosine kinases, VEGFR-2, Flt-3, PDGFR-β, c-Kit, and EGFR. Structure-activity relationship studies indicated that electron-donating groups on the phenyl ring at the 3-position of pyrimidine-2,4,6-trione were required to increase the electron density on the 5-(aminomethylene)pyrimidine-2,4,6-trione moiety.