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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,*
1 Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, China 2 State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, China 3 Center of Drug Discovery, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, China These authors contributed equally to this work.
* Authors to whom correspondence should be addressed.
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 (CC BY 3.0).
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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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