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1,2-Bis(methylsulfonyl)-1-(2-chloroethyl)-2-[(methylamino)carbonyl]hydrazine (VNP40101M): I. Direct inhibition of O6-alkylguanine-DNA alkyltransferase (AGT) by electrophilic species generated by decomposition.
Penketh PG, Shyam K, Baumann RP, Remack JS, Brent TP, Sartorelli AC. Penketh PG, et al. Among authors: baumann rp. Cancer Chemother Pharmacol. 2004 Apr;53(4):279-87. doi: 10.1007/s00280-003-0740-7. Epub 2003 Dec 24. Cancer Chemother Pharmacol. 2004. PMID: 14704831
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 tumor cell resistance.
Baumann RP, Penketh PG, Ishiguro K, Shyam K, Zhu YL, Sartorelli AC. Baumann RP, et al. Biochem Pharmacol. 2010 Jun 1;79(11):1553-61. doi: 10.1016/j.bcp.2009.12.004. Epub 2009 Dec 11. Biochem Pharmacol. 2010. PMID: 20005211 Free PMC article.
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 properties.
Penketh PG, Baumann RP, Shyam K, Williamson HS, Ishiguro K, Zhu R, Eriksson ES, Eriksson LA, Sartorelli AC. Penketh PG, et al. Among authors: baumann rp. Chem Biol Drug Des. 2011 Oct;78(4):513-26. doi: 10.1111/j.1747-0285.2011.01193.x. Epub 2011 Sep 6. Chem Biol Drug Des. 2011. PMID: 21777394 Free PMC article.
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.
Zhu R, Liu MC, Luo MZ, Penketh PG, Baumann RP, Shyam K, Sartorelli AC. Zhu R, et al. Among authors: baumann rp. J Med Chem. 2011 Nov 10;54(21):7720-8. doi: 10.1021/jm201115f. Epub 2011 Oct 17. J Med Chem. 2011. PMID: 21955333 Free PMC article.
110 results