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Items: 1 to 20 of 246

1.

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
2.

Structural analysis of DFG-in and DFG-out dual Src-Abl inhibitors sharing a common vinyl purine template.

Zhou T, Commodore L, Huang WS, Wang Y, Sawyer TK, Shakespeare WC, Clackson T, Zhu X, Dalgarno DC.

Chem Biol Drug Des. 2010 Jan;75(1):18-28. doi: 10.1111/j.1747-0285.2009.00905.x. Epub 2009 Nov 5.

PMID:
19895503
3.

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
4.

C6-unsubstituted pyrazolo[3,4-d]pyrimidines are dual Src/Abl inhibitors effective against imatinib mesylate resistant chronic myeloid leukemia cell lines.

Santucci MA, Corradi V, Mancini M, Manetti F, Radi M, Schenone S, Botta M.

ChemMedChem. 2009 Jan;4(1):118-26. doi: 10.1002/cmdc.200800320.

PMID:
19039816
5.
6.

Activity of FB2, a novel dual Abl/Src tyrosine kinase inhibitor, against imatinib-resistant chronic myeloid leukemia in vivo and in vitro.

Liu H, Li H, Feng Z, Tai J, Meng Y, Wang H, Xin H, Zhang S, Zuo M, Zhang Y, Chen X.

Leuk Lymphoma. 2009 Mar;50(3):437-46. doi: 10.1080/10428190802709438.

PMID:
19347730
7.

Dual Src and Abl inhibitors target wild type Abl and the AblT315I Imatinib-resistant mutant with different mechanisms.

Crespan E, Radi M, Zanoli S, Schenone S, Botta M, Maga G.

Bioorg Med Chem. 2010 Jun 1;18(11):3999-4008. doi: 10.1016/j.bmc.2010.04.024. Epub 2010 Apr 18.

PMID:
20451394
8.

Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations.

Seeliger MA, Ranjitkar P, Kasap C, Shan Y, Shaw DE, Shah NP, Kuriyan J, Maly DJ.

Cancer Res. 2009 Mar 15;69(6):2384-92. doi: 10.1158/0008-5472.CAN-08-3953. Epub 2009 Mar 10.

9.

Characterization of compound 584, an Abl kinase inhibitor with lasting effects.

Puttini M, Redaelli S, Moretti L, Brussolo S, Gunby RH, Mologni L, Marchesi E, Cleris L, Donella-Deana A, Drueckes P, Sala E, Lucchini V, Kubbutat M, Formelli F, Zambon A, Scapozza L, Gambacorti-Passerini C.

Haematologica. 2008 May;93(5):653-61. doi: 10.3324/haematol.12212. Epub 2008 Mar 26.

10.

Last findings on dual inhibitors of abl and SRC tyrosine-kinases.

Schenone S, Manetti F, Botta M.

Mini Rev Med Chem. 2007 Feb;7(2):191-201. Review.

PMID:
17305593
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.

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
13.

Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.

Huang H, Ma J, Shi J, Meng L, Jiang H, Ding J, Liu H.

Bioorg Med Chem. 2010 Jul 1;18(13):4615-24. doi: 10.1016/j.bmc.2010.05.032. Epub 2010 May 19.

PMID:
20570525
14.

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
15.

Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

Lombardo LJ, Lee FY, Chen P, Norris D, Barrish JC, Behnia K, Castaneda S, Cornelius LA, Das J, Doweyko AM, Fairchild C, Hunt JT, Inigo I, Johnston K, Kamath A, Kan D, Klei H, Marathe P, Pang S, Peterson R, Pitt S, Schieven GL, Schmidt RJ, Tokarski J, Wen ML, Wityak J, Borzilleri RM.

J Med Chem. 2004 Dec 30;47(27):6658-61.

PMID:
15615512
16.

3D-QSAR studies on c-Src kinase inhibitors and docking analyses of a potent dual kinase inhibitor of c-Src and c-Abl kinases.

Thaimattam R, Daga PR, Banerjee R, Iqbal J.

Bioorg Med Chem. 2005 Aug 1;13(15):4704-12.

PMID:
15914012
17.

Synthetic SRC-kinase domain inhibitors and their structural requirements.

Schenone S, Manetti F, Botta M.

Anticancer Agents Med Chem. 2007 Nov;7(6):660-80.

PMID:
18045061
18.

Exploration of (S)-3-aminopyrrolidine as a potentially interesting scaffold for discovery of novel Abl and PI3K dual inhibitors.

Zhang C, Tan C, Zu X, Zhai X, Liu F, Chu B, Ma X, Chen Y, Gong P, Jiang Y.

Eur J Med Chem. 2011 Apr;46(4):1404-14. doi: 10.1016/j.ejmech.2011.01.020. Epub 2011 Jan 21.

PMID:
21295380
19.

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
20.

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
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