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Molecules 2012, 17(6), 7556-7568; doi:10.3390/molecules17067556
Article

Synthesis and Biological Evaluation of Novel Furozan-Based Nitric Oxide-Releasing Derivatives of Oridonin as Potential Anti-Tumor Agents

1,2,†, 1,3,†, 1, 2,3,*  and 1,2,*
Received: 25 April 2012 / Revised: 8 June 2012 / Accepted: 12 June 2012 / Published: 18 June 2012
(This article belongs to the collection Bioactive Compounds)
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Abstract

To search for novel nitric oxide (NO) releasing anti-tumor agents, a series of novel furoxan/oridonin hybrids were designed and synthesized. Firstly, the nitrate/nitrite levels in the cell lysates were tested by a Griess assay and the results showed that these furoxan-based NO-releasing derivatives could produce high levels of NO in vitro. Then the anti-proliferative activity of these hybrids against four human cancer cell lines was also determined, among which, 9h exhibited the most potential anti-tumor activity with IC50 values of 1.82 µM against K562, 1.81 µM against MGC-803 and 0.86 µM against Bel-7402, respectively. Preliminary structure-activity relationship was concluded based on the experimental data obtained. These results suggested that NO-donor/natural product hybrids may provide a promising approach for the discovery of novel anti-tumor agents.
Keywords: NO donor; oridonin; hybrid; anti-tumor agents; SAR NO donor; oridonin; hybrid; anti-tumor agents; SAR
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.

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Li, D.; Wang, L.; Cai, H.; Zhang, Y.; Xu, J. Synthesis and Biological Evaluation of Novel Furozan-Based Nitric Oxide-Releasing Derivatives of Oridonin as Potential Anti-Tumor Agents. Molecules 2012, 17, 7556-7568.

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