| Literature DB >> 26807764 |
Vellekkatt Jamsheena1, Ganesan Shilpa2, Jayaram Saranya3, Nissy Ann Harry3, Ravi Shankar Lankalapalli4, Sulochana Priya5.
Abstract
Bis(indolyl)methane appended biaryls were designed, synthesized and evaluated in human cervical cancer cell lines (HeLa) for their anticancer activities and compared against normal rat cardiac myoblasts (H9C2) cells. Compounds 1-12 were synthesized, with variations in one of the phenyl unit, in a single step by condensation of biaryl-2-carbaldehydes with indole in the presence of para-toluenesulfonic acid. Compound 1 exhibited a GI50 value of 11.00 ± 0.707 μM and the derivatives, compounds 4 and 11 showed a GI50 value of 8.33 ± 0.416 μM and 9.13 ± 0.177 μM respectively in HeLa cells and was found to be non-toxic to H9C2 cells up to 20 μM. Furthermore, compounds 1, 4 and 11 induced caspase dependent cellular apoptosis in a concentration-dependent manner, reduced mitochondrial membrane potential, inhibited the cell migration and downregulated the production of MMP-2 and MMP-9 in HeLa cells.Entities:
Keywords: Apoptosis; Biaryl; Bis(indolyl)methane; H9C2 cells; HeLa cells; Matrix metalloproteinases
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Year: 2016 PMID： 26807764 DOI： 10.1016/j.cbi.2016.01.017
Source DB: PubMed Journal: Chem Biol Interact ISSN： 0009-2797 Impact factor: 5.192