929683-54-5Relevant academic research and scientific papers
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.
4-heterocycle substituted quinazoline derivative and preparation method and application thereof
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Paragraph 0041; 0047; 0049; 0051, (2020/02/19)
The invention discloses a 4-heterocycle substituted quinazoline derivative and a preparation method and application thereof. The compound has a structure expressed by a general formula (I): (please see the specification for the formula), in the formula, R1 and R2 are independently selected from hydrogen, a saturated or unsaturated five-membered heterocycle, or a saturated or unsaturated six-membered heterocycle, and n is an integer from 1 to 6; X is NH, O or S; and a heterocycle A is independently selected from pyridine or substituted pyridine, pyrimidine or substituted pyrimidine, pyrazol orsubstituted pyrazol, pyrazine or substituted pyrazine, thiazole or substituted thiazole, or benzothiazole or substituted benzothiazole. The compound or pharmaceutically formable salts thereof have aninhibitory effect on proliferation of tumor cells and can be used for preparing drugs for treatment of glioma, non-small cell lung cancer, breast cancer, colon cancer, stomach cancer, liver cancer andcervical cancer diseases.
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 and spectroscopic characterisation of novel roflumilast analogues
Sun, Gangchun,Si, Yuhui,Song, Ge,Mai, Wenpeng,Li, Zhicheng
, p. 583 - 585 (2013/11/06)
A series of new N-heterocyclic or phenoxy substituted roflumilast analogues have been designed and synthesised. N-heterocyclic or phenoxy substituted benzaldehydes were first prepared from 3-hydroxy-4-methoxybenzaldehbyde and 1-bromo-3-chloropropane by an
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
Synthesis of a new series of 1H-imidazol-1-yl substituted 8-phenylxanthines as adenosine receptor ligands
Bansal, Ranju,Kumar, Gulshan,Gandhi, Deepika,Young, Louise C.,Harvey, Alan L.
experimental part, p. 1290 - 1300 (2012/08/28)
A new series of 1H-imidazol-1-yl substituted 8-phenylxanthine analogs has been synthesized to study the effects of the imidazole group on the binding affinity of compounds for adenosine receptors. Competition binding studies of these compounds were carrie
