Synthesis of antitumor 3,4,6,7-tetrahydro-2H-pyrimido[1,6-c]quinazolin-2-imine derivatives via reductive dearomatization-initiated intramolecular cyclization

被引：2

作者：

Li, Wei ^{[1
,4
]}

Zhou, Xiaotian ^{[3
]}

Chen, Yang ^{[2
]}

Guo, Shunmin ^{[4
]}

Ba, Feifei ^{[2
]}

Tian, Wei ^{[1
]}

Yang, Chao ^{[1
]}

Wang, Mingping ^{[1
]}

Liu, Yu ^{[1
]}

Song, Yunlong ^{[1
]}

Zhu, Ju ^{[1
]}

Zhou, Youjun ^{[1
]}

Zhou, Feng ^{[1
,3
]}

Guo, Hao ^{[2
]}

Zheng, Canhui ^{[1
]}

机构：

[1] Second Mil Med Univ, Sch Pharm, Shanghai 200433, Peoples R China

[2] Fudan Univ, Dept Chem, Shanghai 200433, Peoples R China

[3] Shanghai Inst Pharmaceut Ind, State Key Lab New Drug & Pharmaceut Proc, Shanghai 200040, Peoples R China

[4] Fujian Acad Med Sci, Fujian Prov Key Lab Med Anal, Fuzhou 350001, Peoples R China

来源：

TETRAHEDRON | 2016年 / 72卷 / 23期

基金：

中国国家自然科学基金; 对外科技合作项目（国际科技项目）;

关键词：

3,4,6,7-Tetrahydro-2H-pyrimido[1,6-c]quinazolin-2-imine; N-fused heterocycles; Cyclization reaction; Antitumor agents; Kinase inhibitors; ENDOTHELIAL GROWTH-FACTOR; NITROGEN-HETEROCYCLES; INHIBITORS; RECEPTOR; CANCER;

D O I：

10.1016/j.tet.2016.04.036

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

In light of the importance of N-fused heterocycles in pharmaceuticals, there is continuing interest in research on N-fused heterocycles and their preparation. A new and efficient reductive dearomatization-initiated intramolecular cyclization reaction with a broad scope has been developed, affording 3,4,6,7-tetrahydro-2H-pyrimido[1,6-c]quinazolin-2-imine derivatives. Notably, this type of compound showed good inhibitory activity against specific kinases and human cancer cell lines. These results might mean a new molecular scaffold for the development of new antitumor agents. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：3185 / 3192

页数：8

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