title: 3-substitued indoles: one-pot synthesis and evaluation of anticancer and Src kinase inhibitory activities.
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)-SiO(2) 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 μM. The unsubstituted phenyl (4d) and 3-nitrophenyl (4l) derivatives showed the inhibition of c-Src kinase with IC(50) values of 50.6 and 58.3 μM, respectively.
authors: Department of Chemistry, Birla Institute of Technology and Science, Pilani, Rajasthan, India.
authors: V Kameshwara
authors: VK
authors: Rao
authors: Bhupender S
authors: BS
authors: Chhikara
authors: Amir Nasrolahi
authors: AN
authors: Shirazi
authors: Rakesh
authors: R
authors: Tiwari
authors: Keykavous
authors: K
authors: Parang
authors: Anil
authors: A
authors: Kumar