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Professor Wenfang Xu
Institute of Medicinal Chemistry, College of Pharmacy
Shandong University
Jinan, 250012, P. R. China
Email: xuwenf@sdu.edu.cn
Tel: +86-531-8382264
Fax: +86-531-8382264

We are interested in synthesis and antitumor activity of the peptidomimetic inhibitors of matrix metalloproteinases (MMPs). MMPs are a family of zinc-dependent endopeptidase involved in the degradation and remodeling the extracellular matrix proteins. It had been proved that the MMPs play key roles in the processes of tumor growth, invasion, metastasis and angiogenesis, and have been associated with an aggressive malignant phenotype and poor prognosis in patients with cancer. Thus it is believed that the growth and metastasis can be controlled by MMP inhibitors (MMPIs) which are expected to be useful for the treatment of cancer.
Base on the 3D structures of known MMPIs and binding modes of these compounds in complex with MMPs, we designed several series peptidomimetic inhibitors of MMPs. Preliminary activity assay was carried out both in vitro and in vivo. Inhibiting activities of compounds on gelatinase (MMP-2 and -9) were measured. In vivo experiment, we used the anti-metastasis model of mice bearing H22 tumor cell to evaluate the inhibiting activities. The results of the test demonstrated that quite a few compounds showed significant anti-MMP activity and anticancer activities among which the pyrrolindine derivatives showed especially high activity and expected to be a kind of novel antitumor lead compounds.

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