Bioorganic & Medicinal Chemistry 2007-10-15

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

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

Index: Bioorg. Med. Chem. 15(20) , 6608-17, (2007)

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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.