FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2106457029> ?p ?o ?g. }

• W2106457029 endingPage "495" @default.
• W2106457029 startingPage "484" @default.
• W2106457029 abstract "Abstract Amonafide, a naphthalimide derivative, although selected for exploratory clinical trials for its potent anticancer activity, has long been challenged by its unpredictable side effects. In the present study, a novel amonafide analogue, 2-(2-dimethylamino)-6-thia-2-aza-benzo-[def]-chrysene-1,3-diones (R16) was synthesized by substituting 5′-NH2 of the naphthyl with a heterocyclic group to amonafide, with additional introduction of a thiol group. In a panel of various human tumor cell lines, R16 was more cytotoxic than its parent compound amonafide. It was also effective against multidrug-resistant cells. Importantly, the i.p. administration of R16 inhibited tumor growth in mice implanted with S-180 sarcoma and H22 hepatoma. The molecular and cellular machinery studies showed that the R16 functions as a topoisomerase II (topo II) poison via binding to the ATPase domain of human topo IIα. The superior cytotoxicity of R16 to amonafide was ascribed to its potent effects on trapping topo II–DNA cleavage complexes. Moreover, using a topo II catalytic inhibitor aclarubicin, ataxia-telangiectasia-mutated (ATM)/ATM- and Rad3-related (ATR) kinase inhibitor caffeine and topo II–deficient HL-60/MX2 cells, we further showed that R16-triggered DNA double-strand breaks, tumor cell cycle arrest, and apoptosis were in a topo II–dependent manner. Taken together, R16 stood out by its improved anticancer activity, appreciable anti–multidrug resistance activities, and well-defined topo II poisoning mechanisms, as comparable with the parent compound amonafide. All these collectively promise the potential value of R16 as an anticancer drug candidate, which deserves further development. [Mol Cancer Ther 2007;6(2):484–95]" @default.
• W2106457029 created "2016-06-24" @default.
• W2106457029 creator A5013917173 @default.
• W2106457029 creator A5024458968 @default.
• W2106457029 creator A5055455443 @default.
• W2106457029 creator A5055540928 @default.
• W2106457029 creator A5061074781 @default.
• W2106457029 creator A5063800558 @default.
• W2106457029 creator A5065472339 @default.
• W2106457029 creator A5079498299 @default.
• W2106457029 creator A5081291550 @default.
• W2106457029 creator A5089348951 @default.
• W2106457029 creator A5089537331 @default.
• W2106457029 creator A5091665347 @default.
• W2106457029 creator A5091869532 @default.
• W2106457029 date "2007-02-01" @default.
• W2106457029 modified "2023-09-30" @default.
• W2106457029 title "R16, a novel amonafide analogue, induces apoptosis and G2-M arrest via poisoning topoisomerase II" @default.
• W2106457029 cites W1592483093 @default.
• W2106457029 cites W1898204010 @default.
• W2106457029 cites W1971967721 @default.
• W2106457029 cites W1982810544 @default.
• W2106457029 cites W1985775217 @default.
• W2106457029 cites W1986621896 @default.
• W2106457029 cites W1987325811 @default.
• W2106457029 cites W1987801675 @default.
• W2106457029 cites W1988749598 @default.
• W2106457029 cites W1996564028 @default.
• W2106457029 cites W2006951127 @default.
• W2106457029 cites W2011345987 @default.
• W2106457029 cites W2018434022 @default.
• W2106457029 cites W2030356635 @default.
• W2106457029 cites W2031472508 @default.
• W2106457029 cites W2034660754 @default.
• W2106457029 cites W2040262279 @default.
• W2106457029 cites W2057900776 @default.
• W2106457029 cites W2069499604 @default.
• W2106457029 cites W2073028327 @default.
• W2106457029 cites W2079651661 @default.
• W2106457029 cites W2080409413 @default.
• W2106457029 cites W2085925430 @default.
• W2106457029 cites W2086401995 @default.
• W2106457029 cites W2089515084 @default.
• W2106457029 cites W2092629964 @default.
• W2106457029 cites W2097173890 @default.
• W2106457029 cites W2102345056 @default.
• W2106457029 cites W2103489107 @default.
• W2106457029 cites W2109689528 @default.
• W2106457029 cites W2122347701 @default.
• W2106457029 cites W2123109886 @default.
• W2106457029 cites W2124624490 @default.
• W2106457029 cites W2125353417 @default.
• W2106457029 cites W2125536365 @default.
• W2106457029 cites W2135599444 @default.
• W2106457029 cites W2154294284 @default.
• W2106457029 cites W2268247975 @default.
• W2106457029 cites W2315386342 @default.
• W2106457029 cites W2341695868 @default.
• W2106457029 doi "https://doi.org/10.1158/1535-7163.mct-06-0584" @default.
• W2106457029 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/17308047" @default.
• W2106457029 hasPublicationYear "2007" @default.
• W2106457029 type Work @default.
• W2106457029 sameAs 2106457029 @default.
• W2106457029 citedByCount "72" @default.
• W2106457029 countsByYear W21064570292012 @default.
• W2106457029 countsByYear W21064570292013 @default.
• W2106457029 countsByYear W21064570292014 @default.
• W2106457029 countsByYear W21064570292015 @default.
• W2106457029 countsByYear W21064570292016 @default.
• W2106457029 countsByYear W21064570292017 @default.
• W2106457029 countsByYear W21064570292018 @default.
• W2106457029 countsByYear W21064570292019 @default.
• W2106457029 countsByYear W21064570292020 @default.
• W2106457029 countsByYear W21064570292021 @default.
• W2106457029 countsByYear W21064570292022 @default.
• W2106457029 crossrefType "journal-article" @default.
• W2106457029 hasAuthorship W2106457029A5013917173 @default.
• W2106457029 hasAuthorship W2106457029A5024458968 @default.
• W2106457029 hasAuthorship W2106457029A5055455443 @default.
• W2106457029 hasAuthorship W2106457029A5055540928 @default.
• W2106457029 hasAuthorship W2106457029A5061074781 @default.
• W2106457029 hasAuthorship W2106457029A5063800558 @default.
• W2106457029 hasAuthorship W2106457029A5065472339 @default.
• W2106457029 hasAuthorship W2106457029A5079498299 @default.
• W2106457029 hasAuthorship W2106457029A5081291550 @default.
• W2106457029 hasAuthorship W2106457029A5089348951 @default.
• W2106457029 hasAuthorship W2106457029A5089537331 @default.
• W2106457029 hasAuthorship W2106457029A5091665347 @default.
• W2106457029 hasAuthorship W2106457029A5091869532 @default.
• W2106457029 hasBestOaLocation W21064570291 @default.
• W2106457029 hasConcept C109316439 @default.
• W2106457029 hasConcept C147897179 @default.
• W2106457029 hasConcept C185592680 @default.
• W2106457029 hasConcept C190283241 @default.
• W2106457029 hasConcept C202751555 @default.
• W2106457029 hasConcept C552990157 @default.
• W2106457029 hasConcept C55493867 @default.
• W2106457029 hasConcept C71240020 @default.

• next