929683-54-5Relevant articles and documents
Design, synthesis, and biological evaluation of quinazoline derivatives containing piperazine moieties as antitumor agents
Li, Wen,Chen, Shu-Yi,Hu, Wei-Nan,Zhu, Mei,Liu, Jia-Min,Fu, Yi-Hong,Wang, Zhen-Chao,OuYang, Gui-Ping
, p. 536 - 542 (2020/03/27)
A series of novel quinazoline derivatives containing piperazine analogs are synthesized via substitution reactions with 6,7-disubstituted 4-chloroquinazoline and benzyl piperazine (amido piperazine). Potent antiproliferative activities are observed against A549, HepG2, K562, and PC-3 with N-(3-chlorophenyl)-2-(4-(7-methoxy-6-(3-morpholino-propoxy)quinazoline-4-yl)piperazine-1-yl)acetamidename C9 showing excellent activity. This active derivative was screened for cell migration ability, proliferation effects, and apoptosis against A549 and PC-3 cells, with the result showing biological activity almost equal to that of the control gefitinib.
Four-membered heterocycles-containing 4-anilino-quinazoline derivatives as epidermal growth factor receptor (EGFR) kinase inhibitors
Zhao, Feng,Lin, Zhaohu,Wang, Feng,Zhao, Weili,Dong, Xiaochun
, p. 5385 - 5388 (2013/09/23)
We report herein the design and synthesis of novel azaspirocycle or azetidine substituted 4-anilinoquinazoline derivatives. The EGFR inhibitory activities and in vitro antitumor potency of these newly synthesized compounds against two lung cancer cell lines HCC827 and A549 were evaluated. Most of the target compounds possess good inhibitory potency. In particular, compounds 21g with 2-oxa-6-azaspiro[3.4]octane substituent was found to possess higher EGFR inhibitory activities and similar antitumor potency comparing to the lead compound gefitinib with improved water solubility.
Synthesis of some imidazolyl-substituted 2-benzylidene indanone derivatives as potent aromatase inhibitors for breast cancer therapy
Bansal, Ranju,Narang, Gaurav,Zimmer, Christina,Hartmann, Rolf W.
experimental part, p. 661 - 669 (2012/05/20)
The synthesis and aromatase inhibitory activity of a new series of 2-benzylidene indanones is presented. The imidazolyl-substituted indanones displayed potent aromatase inhibitory activity. The vanilloid-based derivative 2-[4-(3-imidazol-1-ylpropoxy)-3-me