Citation: Pan Xiaole, Wang Lei, Dun Yanyan, Fang Hao. Synthesis and Antiproliferative Activity Studies on 2-Substitued Aniline Quinazoline Derivatives[J]. Chinese Journal of Organic Chemistry, ;2016, 36(5): 1044-1050. doi: 10.6023/cjoc201510018 shu

Synthesis and Antiproliferative Activity Studies on 2-Substitued Aniline Quinazoline Derivatives

1.
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Ji'nan 250012

Corresponding author: Fang Hao, haofangcn@sdu.edu.cn
Received Date: 16 October 2015
Revised Date: 3 January 2016

Fund Project: Project supported by the National Natural Science Foundation of China No.81373281

Figures(2)

A series of 2-substituted aniline quinazoline derivatives were prepared with the starting material of quinazoline-2,4(1H,3H)-dione, and then followed by the reaction of chlorination, Suzuki reaction and nucleophilic substitution. The structures of target compounds were identified by ¹H NMR, ¹³C NMR and HRMS. The preliminary biological evaluations were performed using thiazolyl blue tetrazolium bromide (MTT) method to test their antiproliferative activities against some tumor cell lines. The results suggest that some compounds have the abilities to inhibit the growth of Hela tumor cell lines, and most potent compounds 4u and 4v alsoexhibit good antiproliferative activities against A549 and MCF-7 tumor cell lines.
- quinazoline derivatives,
- antitumor activity,
- synthesis
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沈阳化工大学材料科学与工程学院沈阳 110142