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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 | Abstract
ISSN: 2161-0444

Medicinal Chemistry
Open Access

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Research Article

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

Jie Liu1,3, Fei Sun1,2, Hengyuan Zhang1,2, Hao Cai1,2, Hequan Yao1,2, Weijia Xie1,2, Jieyun Jiang4, Xiaoming Wu1,2 and Jinyi Xu1,2*

1State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China

2Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China

3Department of Organic Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing, 210009, PR China

4Department of Microbiology, Immunology and Molecular Genetics, University of Kentucky College of Medicine, 800 Rose Street, Lexington, KY 40536, USA

*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.

Abstract

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.

Keywords

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