Zhejiang Zhenyuan Pharmaceuticals

Shaoxing, China

Zhejiang Zhenyuan Pharmaceuticals

Shaoxing, China
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Deng L.,Shaoxing University | Yong Z.,Shaoxing University | Tao W.,Zhejiang Supor Pharmaceuticals | Shen J.,Zhejiang Zhenyuan Pharmaceuticals | Wang W.,Zhejiang Supor Pharmaceuticals
Journal of Heterocyclic Chemistry | Year: 2011

Figure represented. Twenty novel norcantharidin derivatives, which were substituted by thiazole ring, were synthesized in a single step by the [3+2] 1,3-dipolar cycloaddition reaction with oxime or hydrazone in the presence of chloramine-T when compared with the conventional method. © 2011 HeteroCorporation.


Hu C.,Shaoxing University | Shen J.,Zhejiang Zhenyuan Pharmaceuticals | Bian K.,Shaoxing University | Zhang R.,Zhejiang University | Deng L.,Shaoxing University
Letters in Drug Design and Discovery | Year: 2014

A series of N1-substituted 2,4,5-triphenyl imidazole derivatives was designed, synthesized and evaluated for their p53-MDM2 binding inhibitory activities and anti-proliferative activities in vitro against four human cancer cell lines (PC3, KB, A549 and HCT116). Although logical evaluation revealed weak p53-MDM2 binding inhibitory activities, most of the obtained molecules displayed moderate to potent cytotoxicities against tested cell lines. As a potential lead compound for further optimization, compound 9c was evaluated as the most potent compound against four cell lines and could induce cell cycle arrest at G2/M phase. The binding mode of compound 9f and MDM2 was further studied by docking analysis and the unexpected interaction mode revealed that this series of compounds may take part into a different binding modes as the lead compound Such as Nutlin, which could induce a different mechanism in cancer therapy. © 2014 Bentham Science Publishers.


Jin Z.,Shaoxing University | Shen J.,Zhejiang Zhenyuan Pharmaceuticals | He J.,Shaoxing University | Hu C.,Shaoxing University
Medicinal Chemistry Research | Year: 2015

p53 is a powerful tumor suppressor, and p53-MDM2 protein-protein interaction has been considered as an attractive cancer therapeutic target. More recently developed small molecules exert their effects by interrupting the p53-MDM2 binding and enhancing the anti-proliferative activities of p53. Small molecules such as Nutlin, MI-63, MI-219, and MI-319 that can activate p53 have shown their anti-tumor effects in different types of malignancies. Drug combinations between p53-MDM2 binding inhibitors with the other anti-proliferative small molecules may allow reduction in the amount of single component with a lower incidence of side effects or better therapeutic effects. In this current review, we present the recent achievements in combination applications between p53-MDM2 binding inhibitors with other small molecules in malignancies. In addition, we discuss how this combination holds promise as a therapeutic strategy for recent and future novel therapies in these diseases. © 2014 Springer Science+Business Media New York.


Deng L.,Shaoxing University | Yong Z.,Shaoxing University | Tao W.,Zhejiang Supor Pharmaceuticals | Shen J.,Zhejiang Zhenyuan Pharmaceuticals | Wang W.,Zhejiang Supor Pharmaceuticals
Journal of Heterocyclic Chemistry | Year: 2011

We use one molecule of ethylene diamine as a connecting arm to combine two molecules of 5,6-dehydronorcantharidin. Then, ten novel norcantharidin derivatives were synthesized in a single step by the [3 + 2] 1,3-dipolar cycloaddition reaction with oxime or hydrazone in the presence of chloramine-T, which is simpler than the conventional method. © 2010 HeteroCorporation.

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