Synthesis and Biological Evaluation of Novel Furozan-Based Nitric Oxide-Releasing Derivatives of 23-Hydroxy Betulinic Acid and 3-oxo-23-hydroxybetulinic acid as Potential Anti-Tumor Agents
- *Corresponding Author:
- Jinyi Xu
Department of Medicinal Chemistry
China Pharmaceutical University
24 Tong Jia Xiang, Nanjing 210009, PR China
Tel: +86 25 83271445
E-mail: [email protected]
Received date: November 21, 2014; Accepted date: January 15, 2015; Published date: January 17, 2015
Citation: Liu J, Sun F, Zhang H, Cai H, Yao H, et al. (2015) Synthesis and Biological Evaluation of Novel Furozan-Based Nitric Oxide-Releasing Derivatives of 23-Hydroxy Betulinic Acid and 3-oxo-23-hydroxybetulinic acid as Potential Anti-Tumor Agents. Med chem 5:028-036. doi:10.4172/2161-0444.1000239
Copyright: © 2015 Liu J, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
To search for novel nitric oxide (NO)-releasing anti-tumor agents, two series of furoxan-based NO-releasing derivatives of 23-Hydroxybetulinic acid and 3-oxo-23-hydroxybetulinic acid were designed and synthesized. The nitrate/nitrite levels in the cell lysates were assayed and the results showed that these derivatives could produce high levels of NO in vitro. Then the antiproliferative activity of these hybrids against four human cancer cell lines was further determined, among which, compound 20a was the most promising derivative with an IC50 under 10 μM on all tested cell lines. The preliminary structure-activity relationships were concluded based on present experimental data.