Reductive 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 tum
about
KS900: A hypoxia-directed, reductively activated methylating antitumor prodrug that selectively ablates O(6)-alkylguanine-DNA alkyltransferase in neoplastic cells.4-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.A strategy for selective O(6)-alkylguanine-DNA alkyltransferase depletion under hypoxic conditions.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 tumorsHypoxia-selective O6-alkylguanine-DNA alkyltransferase inhibitors: design, synthesis, and evaluation of 6-(benzyloxy)-2-(aryldiazenyl)-9H-purines as prodrugs of O6-benzylguanine.Preliminary studies with a new hypoxia-selective cytotoxin, KS119W, in vitro and in vivo.Investigation of tumor hypoxia using a two-enzyme system for in vitro generation of oxygen deficiency.Key role of hydrazine to the interaction between oxaloacetic against phosphoenolpyruvic carboxykinase (PEPCK): ONIOM calculations.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.Hypoxia-activated prodrugs and redox-responsive nanocarriers
P2860
Q34883553-00BE9BC0-2803-4D24-9565-E84E0E260936Q35561443-9ACE4726-3117-493F-99F8-2548B0BC5A4DQ36103542-8F4A4AE7-B8AD-4475-B80B-D86D81E186BAQ36674877-E21F18A8-3532-42D8-B7E4-83257BF2A871Q36865227-95BE442C-9083-4627-8BE5-90069B2BBBD8Q37044152-672F8E7E-5B5E-4214-9382-EFF61597AE23Q39302741-13C17CCC-57BF-4942-973A-12FA16894BB1Q39561817-211366B3-BE64-435B-9456-C806555B37FBQ44285867-5794326B-A150-478B-A291-33EE7EACDB81Q46346689-1B4122C7-0D96-414D-BD81-BE0CBF9BC988Q58694676-87E39C3E-E3E3-4F1F-BFF4-1302CBA5E56C
P2860
Reductive 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 tum
description
2009 nî lūn-bûn
@nan
2009 թուականի Դեկտեմբերին հրատարակուած գիտական յօդուած
@hyw
2009 թվականի դեկտեմբերին հրատարակված գիտական հոդված
@hy
2009年の論文
@ja
2009年論文
@yue
2009年論文
@zh-hant
2009年論文
@zh-hk
2009年論文
@zh-mo
2009年論文
@zh-tw
2009年论文
@wuu
name
Reductive activation of the pr ...... transferase mediated KS119 tum
@ast
Reductive activation of the pr ...... transferase mediated KS119 tum
@en
type
label
Reductive activation of the pr ...... transferase mediated KS119 tum
@ast
Reductive activation of the pr ...... transferase mediated KS119 tum
@en
prefLabel
Reductive activation of the pr ...... transferase mediated KS119 tum
@ast
Reductive activation of the pr ...... transferase mediated KS119 tum
@en
P2093
P2860
P1476
Reductive activation of the pr ...... transferase mediated KS119 tum
@en
P2093
Alan C Sartorelli
Kimiko Ishiguro
Krishnamurthy Shyam
Philip G Penketh
Raymond P Baumann
Yong L Zhu
P2860
P304
P356
10.1016/J.BCP.2009.12.004
P407
P577
2009-12-11T00:00:00Z