title: Anticancer activity of synthetic bis(indolyl)methane-ortho-biaryls against human cervical cancer (HeLa) cells.
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.
authors.affiliation: Academy of Scientific and Innovative Research (AcSIR), New Delhi 110001, India; Chemical Sciences and Technology Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, Kerala, India.
authors.forename: Vellekkatt
authors.initials: V
authors.lastname: Jamsheena
authors.affiliation: Academy of Scientific and Innovative Research (AcSIR), New Delhi 110001, India; Agroprocessing and Natural Products Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, Kerala, India.
authors.forename: Ganesan
authors.initials: G
authors.lastname: Shilpa
authors.affiliation: Agroprocessing and Natural Products Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, Kerala, India.
authors.forename: Jayaram
authors.initials: J
authors.lastname: Saranya
authors.affiliation: Agroprocessing and Natural Products Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, Kerala, India.
authors.forename: Nissy Ann
authors.initials: NA
authors.lastname: Harry
authors.affiliation: Academy of Scientific and Innovative Research (AcSIR), New Delhi 110001, India; Chemical Sciences and Technology Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, Kerala, India. Electronic address: ravishankar@niist.res.in.
authors.forename: Ravi Shankar
authors.initials: RS
authors.lastname: Lankalapalli
authors.affiliation: Academy of Scientific and Innovative Research (AcSIR), New Delhi 110001, India; Agroprocessing and Natural Products Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, Kerala, India. Electronic address: priyasulu@niist.res.in.
authors.forename: Sulochana
authors.initials: S
authors.lastname: Priya
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D005260:Female; D006367:HeLa Cells; D006801:Humans; D007211:Indoles / Q000494:pharmacology*; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects; D002583:Uterine Cervical Neoplasms / Q000473:pathology*
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles
keywords: Apoptosis; Biaryl; Bis(indolyl)methane; H9C2 cells; HeLa cells; Matrix metalloproteinases