Synthesis and bioactivities of 6,7,8-trimethoxy-N-aryl-4-aminoquinazoline derivatives

Bioorg Med Chem. 2007 Oct 15;15(20):6608-17. doi: 10.1016/j.bmc.2007.07.006.

Gang Liu ¹, De-Yu Hu, Lin-Hong Jin, Bao-An Song, Song Yang, Ping-Shen Liu, Pinaki S Bhadury, Yao Ma, Hui Luo, Xian Zhou

Affiliations

Affiliation

1 Center for Research and Development of Fine Chemicals, Key Laboratory of Green Pesticide and Bioengineering, Ministry of Education, Key Laboratory of Fine Chemicals of Guizhou Province, Guizhou University, Guiyang 550025, PR China.

PMID: 17681471 DOI: 10.1016/j.bmc.2007.07.006

Abstract

A series of 4-aminoquinazoline derivatives is prepared by the nucleophilic substitution reaction of 6,7,8-trimethoxy-4-chloroquinazoline and aryl amine. The structures of the compounds are confirmed by elemental analysis, IR, and (1)H NMR spectral data. The compounds are also evaluated for their ability to inhibit tumor cells PC3, A431, Bcap-37, and BGC823 by MTT assays. Among them, 6b and 6e are found as potent inhibitors, with IC(50) values ranging from 5.8 to 9.8microM, in vitro assay.

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