期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 12, 页码 3511-3514出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.05.010
关键词
Anticancer; Cancer; Indole; One-pot; Src kinase; Synthesis
资金
- University Grant Commission (UGC), New Delhi
- American Cancer Society [RSG-07-290-01-CDD]
An efficient and economical method was developed for the synthesis of 3-substituted indoles by one-pot three-component coupling reaction of a substituted or unsubstituted benzaldehyde, N-methylaniline, and indole or N-methylindole using Yb(OTf)(3)-SiO2 as a catalyst. All the synthesized compounds were evaluated for inhibition of cell proliferation of human colon carcinoma (HT-29), human ovarian adenocarcinoma (SK-OV-3), and c-Src kinase activity. The 4-methylphenyl (4o and 4p) and 4-methoxyphenyl (4q) indole derivatives inhibited the cell proliferation of SK-OV-3 and HT-29 cells by 70-77% at a concentration of 50 mu M. The unsubstituted phenyl (4d) and 3-nitrophenyl (4l) derivatives showed the inhibition of c-Src kinase with IC50 values of 50.6 and 58.3 mu M, respectively. (C) 2011 Elsevier Ltd. All rights reserved.
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