Anti-angiogenic activity of basic-type, selective cyclooxygenase (COX)-1 inhibitors

• Published in: Bioorganic & medicinal chemistry letters Vol. 16; no. 11; pp. 3068 - 3072
• Main Authors: Sano, Hiroko, Noguchi, Tomomi, Miyajima, Atsushi, Hashimoto, Yuichi, Miyachi, Hiroyuki
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 01.06.2006; Elsevier
• Subjects: Angiogenesis; Angiogenesis Inhibitors - chemical synthesis; Angiogenesis Inhibitors - chemistry; Angiogenesis Inhibitors - pharmacology; Antineoplastic agents; Biological and medical sciences; Cells, Cultured; COX-1; COX-1 inhibitor; Cyclooxygenase 1 - metabolism; Cyclooxygenase Inhibitors - chemical synthesis; Cyclooxygenase Inhibitors - chemistry; Cyclooxygenase Inhibitors - pharmacology; Endothelial Cells - drug effects; General aspects; Humans; HUVEC; Medical sciences; Molecular Structure; Pharmacology. Drug treatments; Structure-Activity Relationship; Umbilical Cord - drug effects; Angiogenesis; HUVEC; COX-1; COX-1 inhibitor; Antineoplastic agent; Endothelial cell; Cyclooxygenase 1; Selectivity; Vascularization; Blood vessel; Neovascularization; Antiangiogenic agent; Chemical synthesis; Human; Enzyme; Enzyme inhibitor; Competitive inhibition; Biological activity; Cyclooxygenase 1 inhibitor; Cell line; Oxidoreductases; Umbilical cord; Indole derivatives; Umbilical vein; Aromatic amine
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2006.02.021

Indole- and indoline-type basic COX-1-selective competitive inhibitors were found to possess anti-angiogenic activity. Indole- and indoline-type basic COX-1-selective competitive inhibitors, 5-amino-1-(3,5-dimethylbenzoyl)-1 H-indole ( 1) and 5-amino-1-(3,5-dimethylphenyl)-2,3-dihydro-1 H-indole ( 2), were found to possess anti-angiogenic activity estimated as a tube formation-inhibition using human umbilical vein endothelial cells (HUVECs).