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Synthesis and Cytotoxic Evaluation of Quinazolin-4(3H)-one Derivatives Bearing Thiocarbamate, Thiourea or N-Methyldithiocarbamate Side Chains

[ Vol. 8 , Issue. 2 ]


Sheng-Li Cao, Hong Xu, Yao Wang, Ji Liao, Jing-Jing Zhang, Zhong-Feng Li, Yan-Wen Guo, Xiao-Rong Li, Xue-Mei Cui and Xingzhi Xu   Pages 163 - 173 ( 11 )


We have previously found that the dithiocarbamate derivatives of quinazolin-4(3H)-one could act as cytotoxic agents against a panel of human tumor cell lines. To investigate the contribution of dithiocarbamate moiety to the cytotoxic activity, three series of novel quinazolin-4(3H)-one derivatives bearing thiocarbamate, thiourea or Nmethyldithiocarbamate side chains were synthesized and tested for their cytotoxic activity against human cancer cell lines A549, MCF-7, HeLa, HT29 and HCT-116 by MTT assay. The results showed that transformation of the dithiocarbamate moiety in lead compound I to thiocarbamate or thiourea led to a decrease or loss of cytotoxic activity. Some N-alkylated analogs of lead compound II preferentially inhibited the proliferation of A549 cells, although their potencies were not improved in comparison with the unalkylated counterparts. The structure-activity relationship obtained in this research will be beneficial for further synthesis and discovery of effective cytotoxic agents.


Cytotoxic activity, Dithiocarbamate, Quinazolin-4(3H)-one, Thiocarbamate, Thiourea, N-Methyldithiocarbamate, antiinflammatory, Nitrogen atom, isosterism


Department of Chemistry, Capital Normal University, Beijing 100048, China.

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