title: Synthesis and Biological Evaluation of Amidinourea and Triazine Congeners as Inhibitors of MDA-MB-231 Human Breast Cancer Cell Proliferation.
abstract: A series of novel amidinourea derivatives was synthesized, and the compounds were evaluated as inhibitors of MDA-MB-231 human breast cancer cell proliferation. In addition, a second series of triazine derivatives designed as rigid congeners of the amidinoureas was synthesized, and the compounds were evaluated for their antiproliferative activity. Among the two series, amidinourea 3 d (N-[N-[8-[[N-(morpholine-4-carbonyl)carbamimidoyl]amino]octyl]carbamimidoyl]morpholine-4-carboxamide) emerged as a potent anticancer hit compound with an IC50value of 0.76 μm, similar to that of tamoxifen.
authors.affiliation: Department of Applied Sciences, Northumbria University, Ellison Building, Ellison Place, NE1 8ST, Newcastle upon Tyne, UK.
authors.forename: Rosemary
authors.initials: R
authors.lastname: Bass
authors.affiliation: Department of Applied Sciences, Northumbria University, Ellison Building, Ellison Place, NE1 8ST, Newcastle upon Tyne, UK.
authors.forename: Sarah
authors.initials: S
authors.lastname: Jenkinson
authors.affiliation: Department of Applied Sciences, Northumbria University, Ellison Building, Ellison Place, NE1 8ST, Newcastle upon Tyne, UK.
authors.forename: Jennifer
authors.initials: J
authors.lastname: Wright
authors.affiliation: Department of Applied Sciences, Northumbria University, Ellison Building, Ellison Place, NE1 8ST, Newcastle upon Tyne, UK.
authors.forename: Tora
authors.initials: T
authors.lastname: Smulders-Srinivasan
authors.affiliation: Department of Applied Sciences, Northumbria University, Ellison Building, Ellison Place, NE1 8ST, Newcastle upon Tyne, UK.
authors.forename: Jamie C
authors.initials: JC
authors.lastname: Marshall
authors.affiliation: Institute of Pharmaceutical Science, King's College London, 150 Stamford Street, SE1 9NH, London, UK.
authors.forename: Daniele
authors.initials: D
authors.lastname: Castagnolo
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D015195:Drug Design; D019791:Guanidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D006146:Guanidines / Q000737:chemistry* / Q000633:toxicity; D006801:Humans; D009025:Morpholines / Q000737:chemistry* / Q000633:toxicity; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity
chemical_list: D000970:Antineoplastic Agents; D006146:Guanidines; D009025:Morpholines; C000620492:N-(N-(8-((N-(morpholine-4-carbonyl)carbamimidoyl)amino)octyl)carbamimidoyl)morpholine-4-carboxamide; D014227:Triazines; C029280:guanidine carboxamide; D014508:Urea; D019791:Guanidine
keywords: MDA-MB-231 cells; amidinoureas; breast cancer; cell proliferation; triazines