53662-46-7Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel 2,4-disubstituted quinazoline derivatives targeting H1975 cells via EGFR-PI3K signaling pathway
Chao, Gao,Dai, Honglin,Ke, Yu,Li, Erdong,Lihong, Shan,Liu, Hongmin,Liu, Limin,Si, Xiaojie,Wang, Zhengjie,Yang, Zhang,Zhang, Luye,Zhang, Qiurong,Zheng, Jiaxin
, (2021/07/28)
In order to find new and highly effective anti-tumor drugs with targeted therapeutic effects, a series of novel 4-aminoquinazoline derivatives containing N-phenylacetamide structure were designed, synthesized and evaluated for antitumor activity against four human cancer cell lines (H1975, PC-3, MDA-MB-231 and MGC-803) using MTT assay. The results showed that the compound 19e had the most potent antiproliferative activity against H1975, PC-3, MDA-MB-231 and MGC-803 cell lines. At the same time, compound 19e could significantly inhibit the colony formation and migration of H1975 cells. Compound 19e also arrested the H1975 cell cycle in the G1 phase and mediated cell apoptosis, promoted the accumulation of ROS in H1975 cells. Furthermore, compound 19e exerted antitumor effect in vitro by reducing the expression of anti-apoptotic protein Bcl-2 and increasing the pro-apoptotic protein Bax and p53. Mechanistically, compound 19e could significantly decreased the phosphorylation of EGFR and its downstream protein PI3K in H1975 cells. Which indicated that compound 19e targeted H1975 cell via interfering with EGFR-PI3K signaling pathway. Molecular docking showed that compound 19e could bind into the active pocket of EGFR. Those work suggested that compound 19e would have remarkable implications for further design of anti-tumor agents.
Copper promoted desulfurization towards the synthesis of isothiocyanates
Mandapati, UshaRani,Pinapati, Srinivasarao,Rudraraju, RameshRaju
supporting information, p. 125 - 128 (2016/12/26)
The cheap, readily available and air stable catalyst was used as the desulfurization agent for the conversion of aniline to isothiocyanates in one pot two step reaction under mild reaction conditions.
Microwave-assisted cyclocondensation for the synthesis of 3-Aryl-2-thioquinazolin-4(3h)-ones
Patil, Suresh,Jadhav,Shejwal,Deshmukh
scheme or table, p. 1858 - 1860 (2012/08/13)
An efficient synthesis of 3-aryl-2-thioquinazolin-4(3H)-one 1a-f is given by the condensation of anthranilic acid and dithiocarbamate triethylammonium salts of substituted aniline in ethanol as solvent under microwave irradiation.
New Heterocyclic Compounds : 5-Oxo/thio-4-aryl-2-phenylimino-1,3,4-dithiazolidines
Jadhav, R. T.,Nimdeokar, N. M.,Paranjpe, M. G.
, p. 970 - 974 (2007/10/02)
5-Oxo/thio-4-aryl-2-phenylimino-1,3,4-dithiazolidines (VI and IX) have been prepared by reaction of S-chloro-N-phenylisothiocarbamoyl chloride and triethylamine salts of arylthiocarbamic acids and aryldithiocarbamic acids respectively.VI and IX when boiled with benzylamine give the same product (XI).The structures of all these products have been assigned on the basis of chemical transformations and IR data.Probable mechanisms of these reactions are also suggested.
