Synthesis and Preliminarily Cytotoxicity to A549, HCT116 and MCF-7 Cell Lines of Thieno[2,3-d]pyrimidine Derivatives Containing Isoxazole Moiety

Jianping Yong; Canzhong Lu; Xiaoyuan Wu

doi:10.20944/preprints201703.0190.v1

Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Version 1 : Received: 24 March 2017 / Approved: 24 March 2017 / Online: 24 March 2017 (17:52:30 CET)

Under the guidance of our previous achievements, and in order to extend this small molecular library. In current work, other 21 novel structures of thieno[2,3-d]pyrimidines containing isoxazole-moiety (1a-1u) were firstly synthesized and the cytotoxicity to A549, HCT116 and MCF-7 cell lines was evaluated using the MTT method. The results showed that most target compounds exhibited good to excellent cytotoxicity to A549, HCT116 and MCF-7 cell lines, especially 6-Methyl-4-{[3-(4-chlorophenyl)-isoxazol-5-yl-]-methoxy-}-thieno[2,3-d]-pyrimidine (1e) exhibited a broad-spectrum and the most potent cytotoxicity to A549, HCT116 and MCF-7 cell lines (IC50s: 2.79, 6.69 and 4.21×10^-3 μM, respectively) as compared with the reference drug gefitinib (IC50s: 17.90, 21.55 and 20.68 μM, respectively). 1e can be seen as the best drug candidates for development of anticancer drugs.

Isoxazole moiety; Thieno[2,3-d]pyrimidine derivatives; Synthesis; Anticancer activity

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Synthesis and Preliminarily Cytotoxicity to A549, HCT116 and MCF-7 Cell Lines of Thieno[2,3-d]pyrimidine Derivatives Containing Isoxazole Moiety

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