期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 8, 页码 2329-2333出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.01.073
关键词
integrins; peptidomimetic; beta-turn; conformations; D-proline
In this paper, we describe the synthesis of a selected library of heterochiral D-Pro-containing RGD-peptidomimetics (RpD) and we investigate the biological activity as inhibitors of fibronectin adhesion to SK-MEL-24 tumor cells. In particular, peptides 4 and 8 showed an IC50 in the 10(-8) M range. Despite the linear structure, the peptides tend to adopt a folded conformation in a polar environment. (c) 2007 Elsevier Ltd. All rights reserved.
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