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dc.contributor.authorHeald, RAen_US
dc.contributor.authorModi, Cen_US
dc.contributor.authorCookson, JCen_US
dc.contributor.authorHutchinson, Ien_US
dc.contributor.authorLaughton, CAen_US
dc.contributor.authorGowan, SMen_US
dc.contributor.authorKelland, LRen_US
dc.contributor.authorStevens, MFGen_US
dc.date.accessioned2018-09-18T14:37:51Z
dc.date.issued2002-01-31en_US
dc.identifier3en_US
dc.identifier.citationJOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 pp. 590 - 597en_US
dc.identifier.issn0022-2623en_US
dc.identifier.urihttps://repository.icr.ac.uk/handle/internal/2778
dc.identifier.doi10.1021/jm011015qen_US
dc.description.abstractTwo short routes to novel methylated pentacyclic quinoacridinium salts have been devised. New compounds display telomerase-inhibitory potency (<1 muM) in the TRAP assay. 3,11-Difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate (12d, RHPS4, NSC 714187) has a higher selectivity for triplex and quadruplex DNA structures than the 3,6,8,11,13-pentamethyl analogue (12c, RHPS3, NSC 714186) and a low overall growth-inhibitory activity in the NCI 60 cell panel (mean GI(50) 13.18 muM); in addition, the activity profile of 12d does not COMPARE with agents of the topoisomerase II class. Compound 12d is soluble in water, stable in the pH range of 5-9, efficiently transported into tumor cells, and is currently the lead structure for further elaboration in this new class of telomerase inhibitor.en_US
dc.format.extent590 - 597en_US
dc.titleAntitumor polycyclic acridines. 8. Synthesis and telomerase-inhibitory activity of methylated pentacyclic acridinium saltsen_US
dc.typeJournal Article
rioxxterms.versionofrecord10.1021/jm011015qen_US
rioxxterms.licenseref.startdate2002-01-31en_US
rioxxterms.typeJournal Article/Reviewen_US
dc.relation.isPartOfJOURNAL OF MEDICINAL CHEMISTRYen_US
pubs.notesresearcherid-numbers: Laughton, Charles/E-5667-2010 orcid-numbers: Laughton, Charles/0000-0003-4090-3960 unique-id: ISI:000173615600006en_US
pubs.notesNot knownen_US
pubs.organisational-group/ICR
pubs.volume45en_US
pubs.embargo.termsNot knownen_US
dc.contributor.icrauthorKelland, Lloyden_US


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