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Page 1
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Zarrinkar PP, Gunawardane RN, Cramer MD, Gardner MF, Brigham D, Belli B, Karaman MW, Pratz KW, Pallares G, Chao Q, Sprankle KG, Patel HK, Levis M, Armstrong RC, James J, Bhagwat SS. Zarrinkar PP, et al. Among authors: bhagwat ss. Blood. 2009 Oct 1;114(14):2984-92. doi: 10.1182/blood-2009-05-222034. Epub 2009 Aug 4. Blood. 2009. PMID: 19654408 Free PMC article.
Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors.
Patel HK, Grotzfeld RM, Lai AG, Mehta SA, Milanov ZV, Chao Q, Sprankle KG, Carter TA, Velasco AM, Fabian MA, James J, Treiber DK, Lockhart DJ, Zarrinkar PP, Bhagwat SS. Patel HK, et al. Among authors: bhagwat ss. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5182-5. doi: 10.1016/j.bmcl.2009.07.024. Epub 2009 Jul 9. Bioorg Med Chem Lett. 2009. PMID: 19646870
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.
Chao Q, Sprankle KG, Grotzfeld RM, Lai AG, Carter TA, Velasco AM, Gunawardane RN, Cramer MD, Gardner MF, James J, Zarrinkar PP, Patel HK, Bhagwat SS. Chao Q, et al. Among authors: bhagwat ss. J Med Chem. 2009 Dec 10;52(23):7808-16. doi: 10.1021/jm9007533. J Med Chem. 2009. PMID: 19754199
CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity.
James J, Ruggeri B, Armstrong RC, Rowbottom MW, Jones-Bolin S, Gunawardane RN, Dobrzanski P, Gardner MF, Zhao H, Cramer MD, Hunter K, Nepomuceno RR, Cheng M, Gitnick D, Yazdanian M, Insko DE, Ator MA, Apuy JL, Faraoni R, Dorsey BD, Williams M, Bhagwat SS, Holladay MW. James J, et al. Among authors: bhagwat ss. Mol Cancer Ther. 2012 Apr;11(4):930-41. doi: 10.1158/1535-7163.MCT-11-0645. Epub 2012 Feb 7. Mol Cancer Ther. 2012. PMID: 22319199
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Rowbottom MW, Faraoni R, Chao Q, Campbell BT, Lai AG, Setti E, Ezawa M, Sprankle KG, Abraham S, Tran L, Struss B, Gibney M, Armstrong RC, Gunawardane RN, Nepomuceno RR, Valenta I, Hua H, Gardner MF, Cramer MD, Gitnick D, Insko DE, Apuy JL, Jones-Bolin S, Ghose AK, Herbertz T, Ator MA, Dorsey BD, Ruggeri B, Williams M, Bhagwat S, James J, Holladay MW. Rowbottom MW, et al. J Med Chem. 2012 Feb 9;55(3):1082-105. doi: 10.1021/jm2009925. Epub 2012 Jan 23. J Med Chem. 2012. PMID: 22168626
4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors.
Holladay MW, Campbell BT, Rowbottom MW, Chao Q, Sprankle KG, Lai AG, Abraham S, Setti E, Faraoni R, Tran L, Armstrong RC, Gunawardane RN, Gardner MF, Cramer MD, Gitnick D, Ator MA, Dorsey BD, Ruggeri BR, Williams M, Bhagwat SS, James J. Holladay MW, et al. Among authors: bhagwat ss. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5342-6. doi: 10.1016/j.bmcl.2011.07.019. Epub 2011 Jul 14. Bioorg Med Chem Lett. 2011. PMID: 21807507
Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.
Abraham S, Hadd MJ, Tran L, Vickers T, Sindac J, Milanov ZV, Holladay MW, Bhagwat SS, Hua H, Ford Pulido JM, Cramer MD, Gitnick D, James J, Dao A, Belli B, Armstrong RC, Treiber DK, Liu G. Abraham S, et al. Among authors: bhagwat ss. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5296-300. doi: 10.1016/j.bmcl.2011.07.027. Epub 2011 Jul 14. Bioorg Med Chem Lett. 2011. PMID: 21802948
Substrate reduction therapy for Krabbe disease and metachromatic leukodystrophy using a novel ceramide galactosyltransferase inhibitor.
Babcock MC, Mikulka CR, Wang B, Chandriani S, Chandra S, Xu Y, Webster K, Feng Y, Nelvagal HR, Giaramita A, Yip BK, Lo M, Jiang X, Chao Q, Woloszynek JC, Shen Y, Bhagwat S, Sands MS, Crawford BE. Babcock MC, et al. Sci Rep. 2021 Jul 14;11(1):14486. doi: 10.1038/s41598-021-93601-1. Sci Rep. 2021. PMID: 34262084 Free PMC article.
Lead identification of a potent benzopyranone selective estrogen receptor modulator.
McKie JA, Bhagwat SS, Brady H, Doubleday M, Gayo L, Hickman M, Jalluri RK, Khammungkhune S, Kois A, Mortensen D, Richard N, Sapienza J, Shevlin G, Stein B, Sutherland M. McKie JA, et al. Among authors: bhagwat ss. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3407-10. doi: 10.1016/j.bmcl.2004.04.081. Bioorg Med Chem Lett. 2004. PMID: 15177442
74 results