127033-73-2Relevant academic research and scientific papers
Synthesis, structure, and biological assay of cinnamic amides as potential EGFR kinase inhibitors
Zhang, Mao,Lu, Xiang,Zhang, Hong-Jia,Li, Na,Xiao, Yu,Zhu, Hai-Liang,Ye, Yong-Hao
, p. 986 - 994 (2013/04/23)
A series of derivatives of cinnamic amide (compounds 2a-2v) were synthesized and evaluated for antiproliferative activities against the human breast cancer cell line MCF-7- and EGFR-inhibitory activities. The structures of compounds 2b and 2i were determined by single-crystal X-ray diffraction analysis. Compounds 2f and 2j showed moderate EGFR inhibitory activity with IC50 values of 5.16 and 7.37 μM, respectively. Docking simulation of compound 2f was carried out to illustrate the binding mode of the molecule into the EGFR active site. Structure-activity relationship analysis found that the N-phenyl rings are required for enhancing the activities.
Synthesis and Biological Evaluation of 2-Styrylquinazolin-4(3H)-ones, a New Class of Antimitotic Anticancer Agents Which Inhibit Tubulin Polymerization
Jiang, J. B.,Hesson, D. P.,Dusak, B. A.,Dexter, D. L.,Kang, G. J.,Hamel, E.
, p. 1721 - 1728 (2007/10/02)
A novel series of 2-styrylquinazolin-4(3H)-ones which inhibited tubulin polymerization and the growth of L1210 murine leukemia cells was discovered.Extensive structure-activity relationship studies suggest that the entire quinazolinone structure was requi
