title: 6-Substituted imidazo[1,2-a]pyridines: synthesis and biological activity against colon cancer cell lines HT-29 and Caco-2.
abstract: A range of 6-substituted imidazo[1,2-a]pyridines were synthesized using a multicomponent coupling reaction. Most of these compounds were found to exhibit excellent activity against the colon cancer cell lines HT-29 and Caco-2, whilst not showing significant toxicity against white blood cells. Our studies have shown that the proteolytic phase of apoptosis was initiated 2 h after treatment with these imidazo-[1,2-a]pyridines. The data suggests that the imidazo[1,2-a]pyridine-induced cell death in HT-29 and Caco-2 cells is mediated via pathway(s) that include the release of cytochrome c from the mitochondria to the cytosol and the activation of caspase 3 and caspase 8.
authors.affiliation: Division of Pharmacology, Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of the Witwatersrand, 7 York Road, Parktown 2193, South Africa.
authors.forename: Nurit
authors.initials: N
authors.lastname: Dahan-Farkas
authors.forename: Candice
authors.initials: C
authors.lastname: Langley
authors.forename: Amanda L
authors.initials: AL
authors.lastname: Rousseau
authors.forename: Dharmendra B
authors.initials: DB
authors.lastname: Yadav
authors.forename: Hajierah
authors.initials: H
authors.lastname: Davids
authors.forename: Charles B
authors.initials: CB
authors.lastname: de Koning
mesh_terms: D018938:Caco-2 Cells; D049109:Cell Proliferation / Q000187:drug effects; D019073:HT29 Cells; D006801:Humans; D006868:Hydrolysis; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D011725:Pyridines