Synthesis of polyhalo 2-aryl-4-aminoquinazolines and 3-amino-1H-indazoles as anticancer agents

Yan Shengjiao; Dong Ying; Peng Qiong; Fan Yingxian; He Nengqin; Zhang Jihong*; Lin Jun*

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Synthesis of polyhalo 2-aryl-4-aminoquinazolines and 3-amino-1H-indazoles as anticancer agents

Yan Shengjiao 1,Dong Ying 2 #,Peng Qiong 3 #,Fan Yingxian 3,He Nengqin 2,Zhang Jihong* 3 #,Lin Jun* 2 * #

1.Key Laboratory of Medicinal Chemistry for Natural Resources (Yunnan University), Ministry of Education, School of Chemical Science and Technology, Yunnan University, KunMing 650091

2.Key Laboratory of Medicinal Chemistry for Natural Resources (Yunnan University), Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China

3.College of Life Science and Technology, Kunming University of Science and Technology, Kunming 650224, PR China

*Correspondence author

#Submitted by

Subject:

Funding: We are grateful to the Specialized Research Fund for the Doctoral Program of Higher Education（No.No 2010531110003）

Opened online: 6 April 2012

Accepted by: none

Citation: Yan Shengjiao,Dong Ying,Peng Qiong.Synthesis of polyhalo 2-aryl-4-aminoquinazolines and 3-amino-1H-indazoles as anticancer agents[OL]. [ 6 April 2012] http://en.paper.edu.cn/en_releasepaper/content/4473518

A series of polyhalo 2-aryl-4-aminoquinazolines 3a~3n were prepared by reacting polyhalo isophthalonitriles 1a~1c with amidine hydrochlorides under basic conditions with good yields (70~93%). Similarly, through the reaction of polyhalo isophthalonitriles 1a~1c with hydrazines to give some novel polyhalo 3-aminoindazoles 5 and 7 with moderate yield (70~87%). The anticancer activities of compounds 3, 5 and 7 were evaluated in vitro against human cell lines SkOV-3, HeLa, U2-OS, A549, and MCF-7. Some compounds showed excellent growth inhibitory activity and 3a was found to be the most potent active molecular, with an IC50 value lower than 3.86 μg/mL against the five tumor cell lines.

Keywords:anticancer agents; aminoquinazoline; aminoindazoles; polyhalo isophthalonitriles

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