Chinese Journal of Organic Chemistry >
Synthesis and Biological Evaluation of Novel N'-Arylmethylene-N-(4-benzoyloxy-thiazole-2-yl) Benzoylhydrazone Derivatives
Received date: 2014-08-29
Revised date: 2014-10-30
Online published: 2014-11-05
Supported by
Project supported by the National Program on Key Basic Research Project (973 Program, No. 2010CB126100), the National Natural Science Foundation of China (Nos. 21172090, 31000867) and the Program for Changjiang Scholars and Innovatives Research Team in University (No. IRT0953).
14 novel N'-arylmethylene-N-(4-benzoyloxy-thiazole-2-yl) benzoylhydrazone derivatives were designed and synthesized by incorporating the activated structural templets of thiazole and acylhydrazone. All the target compounds were characterized by 1H NMR, IR, mass spectrometry and elemental analysis, and some of the compounds were confirmed by 13C NMR. Anti-tumor test results showed that the hydrazone compounds showed significant anti-tumor activity. These compounds were more active against the KB cell lines than the CNE2 cell lines. All synthesized compounds were screened by plate method in vitro for their fungicidal activity against Gibberella zeae, Thanatephorus cucumeris, Botrytis cinereapers, Alternaria solani, Alternaria alternate, and Colletotrichum orbiculare. In the 1.0×10－4 g/mL concentration, some tested compounds exhibited middle-inhibitory activity of funguses.
Key words： thiazole; acylhydrazone; anticancer; fungicide
Liu Jianchao , Liu Yongjun , He Hongwu . Synthesis and Biological Evaluation of Novel N'-Arylmethylene-N-(4-benzoyloxy-thiazole-2-yl) Benzoylhydrazone Derivatives[J]. Chinese Journal of Organic Chemistry, 2015 , 35(2) : 462 -466 . DOI: 10.6023/cjoc201408036
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