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Items: 26

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.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3743-8. doi: 10.1016/j.bmcl.2011.04.060. Epub 2011 Apr 22.

PMID:
21561767
2.

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.

J Med Chem. 2010 Jun 24;53(12):4701-19. doi: 10.1021/jm100395q.

PMID:
20513156
3.

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.

Cancer Cell. 2009 Nov 6;16(5):401-12. doi: 10.1016/j.ccr.2009.09.028.

4.

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.

J Med Chem. 2009 Aug 13;52(15):4743-56. doi: 10.1021/jm900166t.

PMID:
19572547
5.

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.

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4907-12. doi: 10.1016/j.bmcl.2008.06.042. Epub 2008 Jun 18.

PMID:
18691885
6.

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.

Chem Biol Drug Des. 2008 Feb;71(2):97-105. doi: 10.1111/j.1747-0285.2007.00615.x. Epub 2008 Jan 3.

PMID:
18179464
7.

SRC inhibitors in metastatic bone disease.

Boyce BF, Xing L, Yao Z, Yamashita T, Shakespeare WC, Wang Y, Metcalf CA 3rd, Sundaramoorthi R, Dalgarno DC, Iuliucci JD, Sawyer TK.

Clin Cancer Res. 2006 Oct 15;12(20 Pt 2):6291s-6295s. Review.

8.

Future anti-catabolic therapeutic targets in bone disease.

Boyce BF, Xing L, Yao Z, Shakespeare WC, Wang Y, Metcalf CA 3rd, Sundaramoorthi R, Dalgarno DC, Iuliucci JD, Sawyer TK.

Ann N Y Acad Sci. 2006 Apr;1068:447-57. Review.

PMID:
16831942
9.

Protein phosphorylation and signal transduction modulation: chemistry perspectives for small-molecule drug discovery.

Sawyer TK, Shakespeare WC, Wang Y, Sundaramoorthi R, Huang WS, Metcalf CA 3rd, Thomas M, Lawrence BM, Rozamus L, Noehre J, Zhu X, Narula S, Bohacek RS, Weigele M, Dalgarno DC.

Med Chem. 2005 May;1(3):293-319. Review.

PMID:
16787325
10.

Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance.

Azam M, Nardi V, Shakespeare WC, Metcalf CA 3rd, Bohacek RS, Wang Y, Sundaramoorthi R, Sliz P, Veach DR, Bornmann WG, Clarkson B, Dalgarno DC, Sawyer TK, Daley GQ.

Proc Natl Acad Sci U S A. 2006 Jun 13;103(24):9244-9. Epub 2006 Jun 5.

11.

Structural basis of Src tyrosine kinase inhibition with a new class of potent and selective trisubstituted purine-based compounds.

Dalgarno D, Stehle T, Narula S, Schelling P, van Schravendijk MR, Adams S, Andrade L, Keats J, Ram M, Jin L, Grossman T, MacNeil I, Metcalf C 3rd, Shakespeare W, Wang Y, Keenan T, Sundaramoorthi R, Bohacek R, Weigele M, Sawyer T.

Chem Biol Drug Des. 2006 Jan;67(1):46-57.

PMID:
16492148
12.

AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes.

Summy JM, Trevino JG, Lesslie DP, Baker CH, Shakespeare WC, Wang Y, Sundaramoorthi R, Metcalf CA 3rd, Keats JA, Sawyer TK, Gallick GE.

Mol Cancer Ther. 2005 Dec;4(12):1900-11.

13.

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.

Blood. 2005 Jul 1;106(1):227-34. Epub 2005 Mar 3.

PMID:
15746079
14.

Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML.

O'Hare T, Pollock R, Stoffregen EP, Keats JA, Abdullah OM, Moseson EM, Rivera VM, Tang H, Metcalf CA 3rd, Bohacek RS, Wang Y, Sundaramoorthi R, Shakespeare WC, Dalgarno D, Clackson T, Sawyer TK, Deininger MW, Druker BJ.

Blood. 2004 Oct 15;104(8):2532-9. Epub 2004 Jul 15.

PMID:
15256422
15.

Structure-based design of novel nonpeptide inhibitors of the Src SH2 domain:phosphotyrosine mimetics exploiting multifunctional group replacement chemistry.

Sundaramoorthi R, Kawahata N, Yang MG, Shakespeare WC, Metcalf CA 3rd, Wang Y, Merry T, Eyermann CJ, Bohacek RS, Narula S, Dalgarno DC, Sawyer TK.

Biopolymers. 2003;71(6):717-29.

PMID:
14991680
16.

Novel bone-targeted Src tyrosine kinase inhibitor drug discovery.

Shakespeare WC, Metcalf CA 3rd, Wang Y, Sundaramoorthi R, Keenan T, Weigele M, Bohacek RS, Dalgarno DC, Sawyer TK.

Curr Opin Drug Discov Devel. 2003 Sep;6(5):729-41. Review.

PMID:
14579523
17.

Bone-targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents.

Vu CB, Luke GP, Kawahata N, Shakespeare WC, Wang Y, Sundaramoorthi R, Metcalf CA 3rd, Keenan TP, Pradeepan S, Corpuz E, Merry T, Bohacek RS, Dalgarno DC, Narula SS, van Schravendijk MR, Ram MK, Adams S, Liou S, Keats JA, Violette SM, Guan W, Weigele M, Sawyer TK.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):3071-4.

PMID:
12941336
18.

Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases.

Wang Y, Metcalf CA 3rd, Shakespeare WC, Sundaramoorthi R, Keenan TP, Bohacek RS, van Schravendijk MR, Violette SM, Narula SS, Dalgarno DC, Haraldson C, Keats J, Liou S, Mani U, Pradeepan S, Ram M, Adams S, Weigele M, Sawyer TK.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):3067-70.

PMID:
12941335
19.

Bone-targeted Src kinase inhibitors: novel pyrrolo- and pyrazolopyrimidine analogues.

Sundaramoorthi R, Shakespeare WC, Keenan TP, Metcalf CA 3rd, Wang Y, Mani U, Taylor M, Liu S, Bohacek RS, Narula SS, Dalgarno DC, van Schravandijk MR, Violette SM, Liou S, Adams S, Ram MK, Keats JA, Weigle M, Sawyer TK, Weigele M.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):3063-6. Erratum in: Bioorg Med Chem Lett. 2003 Dec 15;13(24):4519.

PMID:
12941334
20.

Novel protein kinase inhibitors: SMART drug design technology.

Sawyer TK, Bohacek RS, Metcalf CA 3rd, Shakespeare WC, Wang Y, Sundaramoorthi R, Keenan T, Narula S, Weigele M, Dalgarno DC.

Biotechniques. 2003 Jun;Suppl:2-10, 12-5. Review. No abstract available.

PMID:
12813899
21.

SRC homology-2 inhibitors: peptidomimetic and nonpeptide.

Sawyer TK, Bohacek RS, Dalgarno DC, Eyermann CJ, Kawahata N, Metcalf CA 3rd, Shakespeare WC, Sundaramoorthi R, Wang Y, Yang MG.

Mini Rev Med Chem. 2002 Oct;2(5):475-88. Review.

PMID:
12370048
22.

A novel phosphotyrosine mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp): exploitation in the design of nonpeptide inhibitors of pp60(Src) SH2 domain.

Kawahata N, Yang MG, Luke GP, Shakespeare WC, Sundaramoorthi R, Wang Y, Johnson D, Merry T, Violette S, Guan W, Bartlett C, Smith J, Hatada M, Lu X, Dalgarno DC, Eyermann CJ, Bohacek RS, Sawyer TK.

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2319-23.

PMID:
11527723
23.

Selective inhibition of Src SH2 by a novel thiol-targeting tricarbonyl-modified inhibitor and mechanistic analysis by (1)H/(13)C NMR spectroscopy.

Sundaramoorthi R, Siedem C, Vu CB, Dalgarno DC, Laird EC, Botfield MC, Combs AB, Adams SE, Yuan RW, Weigele M, Narula SS.

Bioorg Med Chem Lett. 2001 Jul 9;11(13):1665-9.

PMID:
11425533
24.

Expression and isolation of antimicrobial small molecules from soil DNA libraries.

MacNeil IA, Tiong CL, Minor C, August PR, Grossman TH, Loiacono KA, Lynch BA, Phillips T, Narula S, Sundaramoorthi R, Tyler A, Aldredge T, Long H, Gilman M, Holt D, Osburne MS.

J Mol Microbiol Biotechnol. 2001 Apr;3(2):301-8.

PMID:
11321587
25.

Structure-based design of an osteoclast-selective, nonpeptide src homology 2 inhibitor with in vivo antiresorptive activity.

Shakespeare W, Yang M, Bohacek R, Cerasoli F, Stebbins K, Sundaramoorthi R, Azimioara M, Vu C, Pradeepan S, Metcalf C 3rd, Haraldson C, Merry T, Dalgarno D, Narula S, Hatada M, Lu X, van Schravendijk MR, Adams S, Violette S, Smith J, Guan W, Bartlett C, Herson J, Iuliucci J, Weigele M, Sawyer T.

Proc Natl Acad Sci U S A. 2000 Aug 15;97(17):9373-8.

26.

Simultaneous assay of Src SH3 and SH2 domain binding using different wavelength fluorescence polarization probes.

Lynch BA, Minor C, Loiacono KA, van Schravendijk MR, Ram MK, Sundaramoorthi R, Adams SE, Phillips T, Holt D, Rickles RJ, MacNeil IA.

Anal Biochem. 1999 Nov 1;275(1):62-73.

PMID:
10542110

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