Author: Robinson, T.P.; Ehlers, T.; Hubbard IV, R.B.; Bai, X.; Arbiser, J.L.; Goldsmith, D.J.; Bowen, J.P.
Description: The quest to find new antitumor compounds is an ongoing research endeavor in many laboratories around the world. The use of small-molecule angiogenesis inhibitors promises to be a potentially effective method for cancer treatment and possible prevention. Many antiangiogenic compounds are in various stages of laboratory evaluations and clinical trials. Curcumin is a natural product that has exhibited potent antiangiogenic properties. Based on a simple pharmacophore model, using standard drug design concepts, aromatic enone and aromatic dienone analogues of curcumin were prepared and/or obtained commercially. These compounds were screened for antiangiogenic properties via an in vitro SVR assay and were found to inhibit cell proliferation.
Subject Headings: Angiogenesis Inhibitors/chemical synthesis/pharmacology; Animals; Antineoplastic Agents/chemical synthesis/pharmacology; Cell Division/drug effects; Cell Line, Transformed; Curcumin/analogs & derivatives/chemical synthesis; Drug Design; Endothelium, Vascular/cytology; Ketones; Mice; Polyenes; Structure-Activity Relationship
Keywords: Design, synthesis, and biological evaluation of angiogenesis inhibitors: aromatic enone and dienone analogues of curcumin
Publication year: 2003
Journal or book title: Bioorganic & Medicinal Chemistry Letters
Volume: 13
Issue: 1
Pages: 115-117
Find the full text :Â https://www.sciencedirect.com/science/article/pii/S0960894X02008326
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Type: Journal Article
Serial number: 2832