title: Preliminary SAR on indole-3-carbinol and related fragments reveals a novel anticancer lead compound against resistant glioblastoma cells.
abstract: The prognosis for glioblastoma patients is, at best, poor, with the median time of survival after diagnosis measured in months. As such, there is much need for the rapid development of potent and novel treatments. Herein, we report our preliminary findings on the SAR of a series of indole-3-carbinol and related fragments and reveal a potent lead with low micromolar activity against a particularly resistant glioblastoma cell culture, providing a new platform for future development of a new therapy in this area.
authors.affiliation: School of Pharmacy and Biomedical Sciences, University of Central Lancashire, Maudland Building, Preston, Lancashire PR1 2HE, UK.
authors.forename: Christopher
authors.initials: C
authors.lastname: Sherer
authors.affiliation: Faculty of Medical Science, Anglia Ruskin University, Bishop Hall Lane, Chelmsford, Essex CM1 1SQ, UK.
authors.forename: Ibrahim
authors.initials: I
authors.lastname: Tolaymat
authors.affiliation: Brain Tumour Research Centre, University of Wolverhampton, Wulfruna Street, Wolverhampton WV1 1LY, UK.
authors.forename: Farzana
authors.initials: F
authors.lastname: Rowther
authors.affiliation: Brain Tumour Research Centre, University of Wolverhampton, Wulfruna Street, Wolverhampton WV1 1LY, UK.
authors.forename: Tracy
authors.initials: T
authors.lastname: Warr
authors.affiliation: School of Pharmacy and Biomedical Sciences, University of Central Lancashire, Maudland Building, Preston, Lancashire PR1 2HE, UK. Electronic address: tjsnape@uclan.ac.uk.
authors.forename: Timothy J
authors.initials: TJ
authors.lastname: Snape
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001932:Brain Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D005909:Glioblastoma / Q000188:drug therapy*; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles; C000621527:bis(2-phenyl-1H-indol-3-yl)methane; C030374:indole; C016517:indole-3-carbinol; C542223:2-phenylindole; C016392:3,3'-diindolylmethane
keywords: 3,3′-Diindoloylmethane; Cancer; Glioblastoma; Indole-3-carbinol; SAR