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Page 1
Mechanism of radiosensitization by the Chk1/2 inhibitor AZD7762 involves abrogation of the G2 checkpoint and inhibition of homologous recombinational DNA repair.
Morgan MA, Parsels LA, Zhao L, Parsels JD, Davis MA, Hassan MC, Arumugarajah S, Hylander-Gans L, Morosini D, Simeone DM, Canman CE, Normolle DP, Zabludoff SD, Maybaum J, Lawrence TS. Morgan MA, et al. Among authors: zabludoff sd. Cancer Res. 2010 Jun 15;70(12):4972-81. doi: 10.1158/0008-5472.CAN-09-3573. Epub 2010 May 25. Cancer Res. 2010. PMID: 20501833 Free PMC article.
Assessment of chk1 phosphorylation as a pharmacodynamic biomarker of chk1 inhibition.
Parsels LA, Qian Y, Tanska DM, Gross M, Zhao L, Hassan MC, Arumugarajah S, Parsels JD, Hylander-Gans L, Simeone DM, Morosini D, Brown JL, Zabludoff SD, Maybaum J, Lawrence TS, Morgan MA. Parsels LA, et al. Among authors: zabludoff sd. Clin Cancer Res. 2011 Jun 1;17(11):3706-15. doi: 10.1158/1078-0432.CCR-10-3082. Epub 2011 Apr 11. Clin Cancer Res. 2011. PMID: 21482692 Free PMC article.
AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies.
Zabludoff SD, Deng C, Grondine MR, Sheehy AM, Ashwell S, Caleb BL, Green S, Haye HR, Horn CL, Janetka JW, Liu D, Mouchet E, Ready S, Rosenthal JL, Queva C, Schwartz GK, Taylor KJ, Tse AN, Walker GE, White AM. Zabludoff SD, et al. Mol Cancer Ther. 2008 Sep;7(9):2955-66. doi: 10.1158/1535-7163.MCT-08-0492. Mol Cancer Ther. 2008. PMID: 18790776
Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors.
Oza V, Ashwell S, Brassil P, Breed J, Ezhuthachan J, Deng C, Grondine M, Horn C, Liu D, Lyne P, Newcombe N, Pass M, Read J, Su M, Toader D, Yu D, Yu Y, Zabludoff S. Oza V, et al. Bioorg Med Chem Lett. 2012 Mar 15;22(6):2330-7. doi: 10.1016/j.bmcl.2012.01.043. Epub 2012 Feb 1. Bioorg Med Chem Lett. 2012. PMID: 22342147
Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.
Oza V, Ashwell S, Almeida L, Brassil P, Breed J, Deng C, Gero T, Grondine M, Horn C, Ioannidis S, Liu D, Lyne P, Newcombe N, Pass M, Read J, Ready S, Rowsell S, Su M, Toader D, Vasbinder M, Yu D, Yu Y, Xue Y, Zabludoff S, Janetka J. Oza V, et al. J Med Chem. 2012 Jun 14;55(11):5130-42. doi: 10.1021/jm300025r. Epub 2012 Jun 4. J Med Chem. 2012. PMID: 22551018
Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors.
Janetka JW, Almeida L, Ashwell S, Brassil PJ, Daly K, Deng C, Gero T, Glynn RE, Horn CL, Ioannidis S, Lyne P, Newcombe NJ, Oza VB, Pass M, Springer SK, Su M, Toader D, Vasbinder MM, Yu D, Yu Y, Zabludoff SD. Janetka JW, et al. Among authors: zabludoff sd. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4242-8. doi: 10.1016/j.bmcl.2008.05.016. Epub 2008 May 6. Bioorg Med Chem Lett. 2008. PMID: 18547806
42 results