Chinese Journal of Organic Chemistry >
Synthesis and Cdc25B Inhibition Activity of Novel Imidazo[2,1-b][1,3,4]thiadiazole Derivatives
Received date: 2013-09-06
Revised date: 2013-10-28
Online published: 2013-11-05
Supported by
Project supported by the Natural Science Foundation of Liaoning Province (No. 20102126).
Researches indicate that the cell division cycle 25 phosphatase B (Cdc25B) is over-expressed in various primary human cancers including breast, colon, cervix, lung, etc. This suggests that the inhibition of Cdc25B may become a promising strategy in oncology. In this work, twenty novel 2,6-diaryl-imidazo[2,1-b][1,3,4]thiadiazoles 4 have been synthesized by microwave-assisted method. Then nineteen novel 2,6-diaryl-imidazo[2,1-b][1,3,4]thiadiazole-5-carbaldehydes (5) have obtained by Vilsmeier-Haack reaction. The structures of new compounds 3, 4 and 5 were characterized by IR, 1H NMR spectra and elemental analysis. The synthesized target compounds 4 and 5 were screened for Cdc25B inhibitory activities. The results revealed that compound 4c showed the highest inhibitory activity against Cdc25B with percentage inhibition 87.68% at 5 μg/mL, compounds 4o and 5c showed moderate activities with percentage inhibition 55.76% and 57.69%, respectively. They can be considered as potential candidates as novel Cdc25B inhibitors.
Key words： imidazo[2,1-b][1,3,4]thiadiazole; microwave-assisted; synthesis; Cdc25B
Li Yingjun , Luo Tongchuan , Jin Kun , Gao Lixin , Shao Xin , Sheng Li , Yu Yang , Li Jia . Synthesis and Cdc25B Inhibition Activity of Novel Imidazo[2,1-b][1,3,4]thiadiazole Derivatives[J]. Chinese Journal of Organic Chemistry, 2014 , 34(2) : 325 -333 . DOI: 10.6023/cjoc201309013
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