Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase
摘要:
We report herein the design and synthesis of novel 4-aminoquinazoline derivatives based on the inhibitors of VEGFR-2 tyrosine kinases. The VEGFR-2 inhibitory activities of these newly synthesized compounds were also evaluated and compared with that of ZD6474. We found that most of target compounds had good inhibitory potency. In particular, compounds 1h, 1n and 1o were found to be 6, 2 and 2-fold more potent than the positive control ZD6474. The leading compound 1h also showed an in vivo activity against HepG2 human tumor xenograft model in BALB/c-nu mice. (C) 2011 Elsevier Ltd. All rights reserved.
DOI:
10.1016/j.bmcl.2011.11.061
作为产物:
描述:
2-氟-4-硝基苯胺 、 氯甲酸三氯甲酯 以
甲苯 为溶剂,
反应 18.0h,
以yielding about 10.9 grams of 2-fluoro-4-nitrophenyl isocyanate的产率得到2-fluoro-4-nitrophenyl isocyanate
MAYTANSINOID DERIVATIVES, CONJUGATES THEREOF, AND METHODS OF USE
申请人:Regeneron Pharmaceuticals, Inc.
公开号:US20170209591A1
公开(公告)日:2017-07-27
Provided herein are maytansinoid compounds, derivatives thereof, conjugates thereof, and methods of treating or preventing proliferative diseases with the same.
Maytansinoid derivatives, conjugates thereof, and methods of use
申请人:Regeneron Pharmaceuticals, Inc.
公开号:US10463749B2
公开(公告)日:2019-11-05
Provided herein are maytansinoid compounds, derivatives thereof, conjugates thereof, and methods of treating or preventing proliferative diseases with the same.