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Chloroethylating and methylating dual function antineoplastic agents display superior cytotoxicity against repair proficient tumor cells.

Zhu R, Baumann RP, Patridge E, Penketh PG, Shyam K, Ishiguro K, Sartorelli AC.

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1853-9. doi: 10.1016/j.bmcl.2013.01.016. Epub 2013 Jan 11.


Mode of action of the chloroethylating and carbamoylating moieties of the prodrug cloretazine.

Ishiguro K, Seow HA, Penketh PG, Shyam K, Sartorelli AC.

Mol Cancer Ther. 2006 Apr;5(4):969-76.


KS900: A hypoxia-directed, reductively activated methylating antitumor prodrug that selectively ablates O(6)-alkylguanine-DNA alkyltransferase in neoplastic cells.

Baumann RP, Ishiguro K, Penketh PG, Shyam K, Zhu R, Sartorelli AC.

Biochem Pharmacol. 2011 May 15;81(10):1201-10. doi: 10.1016/j.bcp.2011.02.019. Epub 2011 Mar 17.


1,2-Bis(methylsulfonyl)-1-(2-chloroethyl)-2-[(methylamino)carbonyl]hydrazine (VNP40101M): II. Role of O6-alkylguanine-DNA alkyltransferase in cytotoxicity.

Baumann RP, Shyam K, Penketh PG, Remack JS, Brent TP, Sartorelli AC.

Cancer Chemother Pharmacol. 2004 Apr;53(4):288-95. Epub 2003 Dec 17.


Role of O6-alkylguanine-DNA alkyltransferase in the cytotoxic activity of cloretazine.

Ishiguro K, Shyam K, Penketh PG, Sartorelli AC.

Mol Cancer Ther. 2005 Nov;4(11):1755-63.


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.

Penketh PG, Patridge E, Shyam K, Baumann RP, Zhu R, Ishiguro K, Sartorelli AC.

Chem Res Toxicol. 2014 Aug 18;27(8):1440-9. doi: 10.1021/tx500197t. Epub 2014 Jul 17.


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.

Cancer Chemother Pharmacol. 2004 Apr;53(4):279-87. Epub 2003 Dec 24.


Quantitative relationship between guanine O(6)-alkyl lesions produced by Onrigin™ and tumor resistance by O(6)-alkylguanine-DNA alkyltransferase.

Ishiguro K, Zhu YL, Shyam K, Penketh PG, Baumann RP, Sartorelli AC.

Biochem Pharmacol. 2010 Nov 1;80(9):1317-25. doi: 10.1016/j.bcp.2010.07.022. Epub 2010 Jul 21.


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 KS119W.

Penketh PG, Shyam K, Zhu R, Baumann RP, Ishiguro K, Sartorelli AC.

Chem Res Toxicol. 2014 May 19;27(5):818-33. doi: 10.1021/tx500004y. Epub 2014 Mar 24.


Expression of mammalian O6-alkylguanine-DNA alkyltransferase in a cell line sensitive to alkylating agents.

Dolan ME, Norbeck L, Clyde C, Hora NK, Erickson LC, Pegg AE.

Carcinogenesis. 1989 Sep;10(9):1613-9.


Preclinical evaluation of Laromustine for use in combination with radiation therapy in the treatment of solid tumors.

Rockwell S, Liu Y, Seow HA, Ishiguro K, Baumann RP, Penketh PG, Shyam K, Akintujoye OM, Glazer PM, Sartorelli AC.

Int J Radiat Biol. 2012 Mar;88(3):277-85. doi: 10.3109/09553002.2012.638359. Epub 2011 Dec 20.


Lethality to leukemia cell lines of DNA interstrand cross-links generated by Cloretazine derived alkylating species.

Penketh PG, Baumann RP, Ishiguro K, Shyam K, Seow HA, Sartorelli AC.

Leuk Res. 2008 Oct;32(10):1546-53. doi: 10.1016/j.leukres.2008.03.005. Epub 2008 May 13.


Design of a hypoxia-activated prodrug inhibitor of O6-alkylguanine-DNA alkyltransferase.

Zhu R, Seow HA, Baumann RP, Ishiguro K, Penketh PG, Shyam K, Sartorelli AC.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6242-7. doi: 10.1016/j.bmcl.2012.08.008. Epub 2012 Aug 10.


Carbamoylating activity associated with the activation of the antitumor agent laromustine inhibits angiogenesis by inducing ASK1-dependent endothelial cell death.

Ji W, Yang M, Praggastis A, Li Y, Zhou HJ, He Y, Ghazvinian R, Cincotta DJ, Rice KP, Min W.

PLoS One. 2014 Jul 28;9(7):e103224. doi: 10.1371/journal.pone.0103224. eCollection 2014.


Laromustine, a sulfonyl hydrolyzing alkylating prodrug for cancer therapy.

Pigneux A.

IDrugs. 2009 Jan;12(1):39-53. Review.


Role of O6-methylguanine-DNA methyltransferase in the resistance of pancreatic tumors to DNA alkylating agents.

Kokkinakis DM, Ahmed MM, Delgado R, Fruitwala MM, Mohiuddin M, Albores-Saavedra J.

Cancer Res. 1997 Dec 1;57(23):5360-8.

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