773130-29-3Relevant academic research and scientific papers
Discovery of novel 4-anilinoquinazoline derivatives as potent inhibitors of epidermal growth factor receptor with antitumor activity
Xu, Yun-Yun,Li, Si-Ning,Yu, Gao-Jian,Hu, Qing-Hua,Li, Huan-Qiu
, p. 6084 - 6091 (2013)
Two new series of new compounds containing a 6-amino-substituted group or 6-acrylamide-substituted group linked to a 4-anilinoquinazoline nucleus have been discovered as potential EGFR inhibitors. These compounds proved efficient effects on antiproliferative activity and EGFR-TK inhibitory activity. Especially, N6-((5-bromothiophen-2-yl)methyl)-N4-(3- chlorophenyl)quinazoline-4,6-diamine (5e), showed the most potent inhibitory activity (IC50 = 3.11 μM for Hep G2, IC50 = 0.82 μM for A549). The EGFR molecular docking model suggested that the new compound is nicely bound to the region of EGFR, and cell morphology by Hoechst stain experiment suggested that these compounds efficiently induced apoptosis of A549 cells.
4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVE OR SALTS THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Paragraph 0173; 0174, (2015/11/16)
The present invention provides a 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt effectively increases the LXR transcriptional activity, and therefore can be usefully applied for preventing or treating a dysfunction in cholesterol metabolism, such as cholesterol gallstone, hyperlipidemia, or coronary atherosclerosis.
