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

doi:10.3390/molecules17067556

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

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

Dahong Li^1,2,†, Lei Wang^1,3,†, Hao Cai¹, Yihua Zhang^2,3,* and Jinyi Xu^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; in revised form: 8 June 2012 / Accepted: 12 June 2012 / Published: 18 June 2012

(This article belongs to the Special Issue 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

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MDPI and ACS Style

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.

AMA Style

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(6):7556-7568.

Chicago/Turabian Style

Li, Dahong; Wang, Lei; Cai, Hao; Zhang, Yihua; Xu, Jinyi. 2012. "Synthesis and Biological Evaluation of Novel Furozan-Based Nitric Oxide-Releasing Derivatives of Oridonin as Potential Anti-Tumor Agents." Molecules 17, no. 6: 7556-7568.

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