Lethality to leukemia cell lines of DNA interstrand cross-links generated by Cloretazine derived alkylating species.
about
Influence of phosphate and phosphoesters on the decomposition pathway of 1,2-bis(methylsulfonyl)-1-(2-chloroethyhydrazine (90CE), the active anticancer moiety generated by Laromustine, KS119, and KS119WReductive activation of the prodrug 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-[[1-(4-nitrophenyl)ethoxy]carbonyl]hydrazine (KS119) selectively occurs in oxygen-deficient cells and overcomes O(6)-alkylguanine-DNA alkyltransferase mediated KS119 tumInhibition of human DNA polymerase beta activity by the anticancer prodrug Cloretazine.Influence of glutathione and glutathione S-transferases on DNA interstrand cross-link formation by 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazine, the active anticancer moiety generated by laromustine.KS900: A hypoxia-directed, reductively activated methylating antitumor prodrug that selectively ablates O(6)-alkylguanine-DNA alkyltransferase in neoplastic cells.1,2-Bis(methylsulfonyl)-1-(2-chloroethyl)-2-[[1-(4-nitrophenyl)ethoxy]carbonyl]hydrazine (KS119): a cytotoxic prodrug with two stable conformations differing in biological and physical properties4-nitrobenzyloxycarbonyl derivatives of O(6)-benzylguanine as hypoxia-activated prodrug inhibitors of O(6)-alkylguanine-DNA alkyltransferase (AGT), which produces resistance to agents targeting the O-6 position of DNA guanine.Thioredoxin reductase is inhibited by the carbamoylating activity of the anticancer sulfonylhydrazine drug laromustine.Chloroethylating and methylating dual function antineoplastic agents display superior cytotoxicity against repair proficient tumor cells.Preclinical evaluation of Laromustine for use in combination with radiation therapy in the treatment of solid tumorsLaromustine (cloretazine).Quantification of DNA interstrand crosslinks induced by ACNU in NIH/3T3 and L1210 cells using high-performance liquid chromatography/electrospray ionization tandem mass spectrometry.pH-dependent general base catalyzed activation rather than isocyanate liberation may explain the superior anticancer efficacy of laromustine compared to related 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazine prodrugs.
P2860
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P2860
Lethality to leukemia cell lines of DNA interstrand cross-links generated by Cloretazine derived alkylating species.
description
2008 nî lūn-bûn
@nan
2008 թուականի Մայիսին հրատարակուած գիտական յօդուած
@hyw
2008 թվականի մայիսին հրատարակված գիտական հոդված
@hy
2008年の論文
@ja
2008年論文
@yue
2008年論文
@zh-hant
2008年論文
@zh-hk
2008年論文
@zh-mo
2008年論文
@zh-tw
2008年论文
@wuu
name
Lethality to leukemia cell lin ...... ne derived alkylating species.
@ast
Lethality to leukemia cell lin ...... ne derived alkylating species.
@en
type
label
Lethality to leukemia cell lin ...... ne derived alkylating species.
@ast
Lethality to leukemia cell lin ...... ne derived alkylating species.
@en
prefLabel
Lethality to leukemia cell lin ...... ne derived alkylating species.
@ast
Lethality to leukemia cell lin ...... ne derived alkylating species.
@en
P2093
P2860
P1433
P1476
Lethality to leukemia cell lin ...... ne derived alkylating species.
@en
P2093
Alan C Sartorelli
Helen A Seow
Kimiko Ishiguro
Krishnamurthy Shyam
Philip G Penketh
Raymond P Baumann
P2860
P304
P356
10.1016/J.LEUKRES.2008.03.005
P577
2008-05-13T00:00:00Z