Document Type
Article
Publication Date
2011
Abstract
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 7077% at a concentration of 50 μM. The unsubstituted phenyl (4d) and 3-nitrophenyl (4l) derivatives showed the inhibition of c-Src kinase with IC50 values of 50.6 μM and 58.3 μM, respectively.
Recommended Citation
Rao, V. Kameshwara, et al. "3-Substitued indoles: one-pot synthesis and evaluation of anticancer and Src kinase inhibitory activities." Bioorganic & medicinal chemistry letters 21.12 (2011): 3511-3514. doi: 10.1016/j.bmcl.2011.05.010
Copyright
Elsevier
Creative Commons License
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Comments
NOTICE: this is the author’s version of a work that was accepted for publication in Bioorganic & Medicinal Chemistry Letters. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in Bioorganic & Medicinal Chemistry Letters, volume 21, issue 12, in 2011. DOI: 10.1016/j.bmcl.2011.05.010
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