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Page 1
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Thomas M, Huang WS, Wen D, Zhu X, Wang Y, Metcalf CA, Liu S, Chen I, Romero J, Zou D, Sundaramoorthi R, Li F, Qi J, Cai L, Zhou T, Commodore L, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Iuliucci J, Rivera VM, Sawyer TK, Dalgarno DC, Clackson T, Shakespeare WC. Thomas M, et al. Among authors: wardwell s. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3743-8. doi: 10.1016/j.bmcl.2011.04.060. Epub 2011 Apr 22. Bioorg Med Chem Lett. 2011. PMID: 21561767
In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and AP23848 against activation-loop mutants of Kit.
Corbin AS, Demehri S, Griswold IJ, Wang Y, Metcalf CA 3rd, Sundaramoorthi R, Shakespeare WC, Snodgrass J, Wardwell S, Dalgarno D, Iuliucci J, Sawyer TK, Heinrich MC, Druker BJ, Deininger MW. Corbin AS, et al. Among authors: wardwell s. Blood. 2005 Jul 1;106(1):227-34. doi: 10.1182/blood-2004-12-4771. Epub 2005 Mar 3. Blood. 2005. PMID: 15746079 Free article.
SAR of carbon-linked, 2-substituted purines: synthesis and characterization of AP23451 as a novel bone-targeted inhibitor of Src tyrosine kinase with in vivo anti-resorptive activity.
Shakespeare WC, Wang Y, Bohacek R, Keenan T, Sundaramoorthi R, Metcalf C 3rd, Dilauro A, Roeloffzen S, Liu S, Saltmarsh J, Paramanathan G, Dalgarno D, Narula S, Pradeepan S, van Schravendijk MR, Keats J, Ram M, Liou S, Adams S, Wardwell S, Bogus J, Iuliucci J, Weigele M, Xing L, Boyce B, Sawyer TK. Shakespeare WC, et al. Among authors: wardwell s. Chem Biol Drug Des. 2008 Feb;71(2):97-105. doi: 10.1111/j.1747-0285.2007.00615.x. Epub 2008 Jan 3. Chem Biol Drug Des. 2008. PMID: 18179464
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.
Wang Y, Shakespeare WC, Huang WS, Sundaramoorthi R, Lentini S, Das S, Liu S, Banda G, Wen D, Zhu X, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Dalgarno D, Clackson T, Sawyer TK. Wang Y, et al. Among authors: wardwell s. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4907-12. doi: 10.1016/j.bmcl.2008.06.042. Epub 2008 Jun 18. Bioorg Med Chem Lett. 2008. PMID: 18691885
9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation.
Huang WS, Zhu X, Wang Y, Azam M, Wen D, Sundaramoorthi R, Thomas RM, Liu S, Banda G, Lentini SP, Das S, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Daley GQ, Iuliucci J, Dalgarno DC, Clackson T, Sawyer TK, Shakespeare WC. Huang WS, et al. Among authors: wardwell s. J Med Chem. 2009 Aug 13;52(15):4743-56. doi: 10.1021/jm900166t. J Med Chem. 2009. PMID: 19572547
AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.
O'Hare T, Shakespeare WC, Zhu X, Eide CA, Rivera VM, Wang F, Adrian LT, Zhou T, Huang WS, Xu Q, Metcalf CA 3rd, Tyner JW, Loriaux MM, Corbin AS, Wardwell S, Ning Y, Keats JA, Wang Y, Sundaramoorthi R, Thomas M, Zhou D, Snodgrass J, Commodore L, Sawyer TK, Dalgarno DC, Deininger MW, Druker BJ, Clackson T. O'Hare T, et al. Among authors: wardwell s. Cancer Cell. 2009 Nov 6;16(5):401-12. doi: 10.1016/j.ccr.2009.09.028. Cancer Cell. 2009. PMID: 19878872 Free PMC article.
Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.
Huang WS, Metcalf CA, Sundaramoorthi R, Wang Y, Zou D, Thomas RM, Zhu X, Cai L, Wen D, Liu S, Romero J, Qi J, Chen I, Banda G, Lentini SP, Das S, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Zhou T, Commodore L, Narasimhan NI, Mohemmad QK, Iuliucci J, Rivera VM, Dalgarno DC, Sawyer TK, Clackson T, Shakespeare WC. Huang WS, et al. Among authors: wardwell s. J Med Chem. 2010 Jun 24;53(12):4701-19. doi: 10.1021/jm100395q. J Med Chem. 2010. PMID: 20513156
Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies.
Gozgit JM, Wong MJ, Wardwell S, Tyner JW, Loriaux MM, Mohemmad QK, Narasimhan NI, Shakespeare WC, Wang F, Druker BJ, Clackson T, Rivera VM. Gozgit JM, et al. Among authors: wardwell s. Mol Cancer Ther. 2011 Jun;10(6):1028-35. doi: 10.1158/1535-7163.MCT-10-1044. Epub 2011 Apr 11. Mol Cancer Ther. 2011. PMID: 21482694 Free PMC article.
29 results