Version 1
: Received: 24 March 2017 / Approved: 24 March 2017 / Online: 24 March 2017 (17:52:30 CET)
How to cite:
Yong, J.; Lu, C.; Wu, X. Synthesis and Preliminarily Cytotoxicity to A549, HCT116 and MCF-7 Cell Lines of Thieno[2,3-d]pyrimidine Derivatives Containing Isoxazole Moiety. Preprints2017, 2017030190 (doi: 10.20944/preprints201703.0190.v1).
Yong, J.; Lu, C.; Wu, X. Synthesis and Preliminarily Cytotoxicity to A549, HCT116 and MCF-7 Cell Lines of Thieno[2,3-d]pyrimidine Derivatives Containing Isoxazole Moiety. Preprints 2017, 2017030190 (doi: 10.20944/preprints201703.0190.v1).
Cite as:
Yong, J.; Lu, C.; Wu, X. Synthesis and Preliminarily Cytotoxicity to A549, HCT116 and MCF-7 Cell Lines of Thieno[2,3-d]pyrimidine Derivatives Containing Isoxazole Moiety. Preprints2017, 2017030190 (doi: 10.20944/preprints201703.0190.v1).
Yong, J.; Lu, C.; Wu, X. Synthesis and Preliminarily Cytotoxicity to A549, HCT116 and MCF-7 Cell Lines of Thieno[2,3-d]pyrimidine Derivatives Containing Isoxazole Moiety. Preprints 2017, 2017030190 (doi: 10.20944/preprints201703.0190.v1).
Abstract
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.
Copyright:
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Jianping Yong