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Results: 1 to 20 of 152

1.

Fragment based discovery of a novel and selective PI3 kinase inhibitor.

Hughes SJ, Millan DS, Kilty IC, Lewthwaite RA, Mathias JP, O'Reilly MA, Pannifer A, Phelan A, Stühmeier F, Baldock DA, Brown DG.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6586-90. doi: 10.1016/j.bmcl.2011.07.117. Epub 2011 Aug 6.

PMID:
21925880
[PubMed - indexed for MEDLINE]
2.

Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases.

Nishiguchi GA, Atallah G, Bellamacina C, Burger MT, Ding Y, Feucht PH, Garcia PD, Han W, Klivansky L, Lindvall M.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6366-9. doi: 10.1016/j.bmcl.2011.08.105. Epub 2011 Sep 10.

PMID:
21945284
[PubMed - indexed for MEDLINE]
3.

Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors.

Pecchi S, Renhowe PA, Taylor C, Kaufman S, Merritt H, Wiesmann M, Shoemaker KR, Knapp MS, Ornelas E, Hendrickson TF, Fantl W, Voliva CF.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):6895-8. doi: 10.1016/j.bmcl.2010.10.021. Epub 2010 Oct 13.

PMID:
21035331
[PubMed - indexed for MEDLINE]
4.

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.

Staben ST, Heffron TP, Sutherlin DP, Bhat SR, Castanedo GM, Chuckowree IS, Dotson J, Folkes AJ, Friedman LS, Lee L, Lesnick J, Lewis C, Murray JM, Nonomiya J, Olivero AG, Plise E, Pang J, Prior WW, Salphati L, Rouge L, Sampath D, Tsui V, Wan NC, Wang S, Weismann C, Wu P, Zhu BY.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):6048-51. doi: 10.1016/j.bmcl.2010.08.067. Epub 2010 Aug 19.

PMID:
20822905
[PubMed - indexed for MEDLINE]
5.

Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration.

Oza V, Ashwell S, Brassil P, Breed J, Deng C, Ezhuthachan J, Haye H, Horn C, Janetka J, Lyne P, Newcombe N, Otterbien L, Pass M, Read J, Roswell S, Su M, Toader D, Yu D, Yu Y, Valentine A, Webborn P, White A, Zabludoff S, Zheng X.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5133-8. doi: 10.1016/j.bmcl.2010.07.015. Epub 2010 Jul 29.

PMID:
20673630
[PubMed - indexed for MEDLINE]
6.

Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases.

McClellan WJ, Dai Y, Abad-Zapatero C, Albert DH, Bouska JJ, Glaser KB, Magoc TJ, Marcotte PA, Osterling DJ, Stewart KD, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5620-4. doi: 10.1016/j.bmcl.2011.06.041. Epub 2011 Jun 29.

PMID:
21778056
[PubMed - indexed for MEDLINE]
7.

Structure-based optimization of morpholino-triazines as PI3K and mTOR inhibitors.

Poulsen A, Williams M, Nagaraj HM, William AD, Wang H, Soh CK, Xiong ZC, Dymock B.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1009-13. doi: 10.1016/j.bmcl.2011.12.001. Epub 2011 Dec 8.

PMID:
22197143
[PubMed - indexed for MEDLINE]
8.

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
[PubMed - indexed for MEDLINE]
9.

Lead optimization and structure-based design of potent and bioavailable deoxycytidine kinase inhibitors.

Jessop TC, Tarver JE, Carlsen M, Xu A, Healy JP, Heim-Riether A, Fu Q, Taylor JA, Augeri DJ, Shen M, Stouch TR, Swanson RV, Tari LW, Hunter M, Hoffman I, Keyes PE, Yu XC, Miranda M, Liu Q, Swaffield JC, David Kimball S, Nouraldeen A, Wilson AG, Foushee AM, Jhaver K, Finch R, Anderson S, Oravecz T, Carson KG.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6784-7. doi: 10.1016/j.bmcl.2009.09.081. Epub 2009 Sep 25.

PMID:
19836232
[PubMed - indexed for MEDLINE]
10.

Fragment based lead discovery of small molecule inhibitors for the EPHA4 receptor tyrosine kinase.

van Linden OP, Farenc C, Zoutman WH, Hameetman L, Wijtmans M, Leurs R, Tensen CP, Siegal G, de Esch IJ.

Eur J Med Chem. 2012 Jan;47(1):493-500. doi: 10.1016/j.ejmech.2011.11.020. Epub 2011 Nov 18.

PMID:
22137457
[PubMed - indexed for MEDLINE]
11.

Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping.

Richardson CM, Nunns CL, Williamson DS, Parratt MJ, Dokurno P, Howes R, Borgognoni J, Drysdale MJ, Finch H, Hubbard RE, Jackson PS, Kierstan P, Lentzen G, Moore JD, Murray JB, Simmonite H, Surgenor AE, Torrance CJ.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3880-5. Epub 2007 May 6.

PMID:
17570665
[PubMed - indexed for MEDLINE]
12.

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
[PubMed - indexed for MEDLINE]
13.

Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.

Furet P, Guagnano V, Fairhurst RA, Imbach-Weese P, Bruce I, Knapp M, Fritsch C, Blasco F, Blanz J, Aichholz R, Hamon J, Fabbro D, Caravatti G.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8. doi: 10.1016/j.bmcl.2013.05.007. Epub 2013 May 14. Erratum in: Bioorg Med Chem Lett. 2013 Aug 15;23(16):4723.

PMID:
23726034
[PubMed - indexed for MEDLINE]
14.

Discovery and in vivo evaluation of dual PI3Kβ/δ inhibitors.

Gonzalez-Lopez de Turiso F, Shin Y, Brown M, Cardozo M, Chen Y, Fong D, Hao X, He X, Henne K, Hu YL, Johnson MG, Kohn T, Lohman J, McBride HJ, McGee LR, Medina JC, Metz D, Miner K, Mohn D, Pattaropong V, Seganish J, Simard JL, Wannberg S, Whittington DA, Yu G, Cushing TD.

J Med Chem. 2012 Sep 13;55(17):7667-85. doi: 10.1021/jm300679u. Epub 2012 Aug 29.

PMID:
22876881
[PubMed - indexed for MEDLINE]
15.

QM/MM as a tool in fragment based drug discovery. A cross-docking, rescoring study of kinase inhibitors.

Gleeson MP, Gleeson D.

J Chem Inf Model. 2009 Jun;49(6):1437-48. doi: 10.1021/ci900022h.

PMID:
19459698
[PubMed - indexed for MEDLINE]
16.

Discovery of MEK/PI3K dual inhibitor via structure-based virtual screening.

Park H, Lee S, Hong S.

Bioorg Med Chem Lett. 2012 Aug 1;22(15):4946-50. doi: 10.1016/j.bmcl.2012.06.041. Epub 2012 Jun 21.

PMID:
22771009
[PubMed - indexed for MEDLINE]
17.

Fragment-based discovery of JAK-2 inhibitors.

Antonysamy S, Hirst G, Park F, Sprengeler P, Stappenbeck F, Steensma R, Wilson M, Wong M.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):279-82. doi: 10.1016/j.bmcl.2008.08.064. Epub 2008 Aug 22.

PMID:
19019674
[PubMed - indexed for MEDLINE]
18.

Structure-based virtual screening of Src kinase inhibitors.

Lee K, Kim J, Jeong KW, Lee KW, Lee Y, Song JY, Kim MS, Lee GS, Kim Y.

Bioorg Med Chem. 2009 Apr 15;17(8):3152-61. doi: 10.1016/j.bmc.2009.02.054. Epub 2009 Mar 5.

PMID:
19321350
[PubMed - indexed for MEDLINE]
19.

Identification of inhibitors of checkpoint kinase 1 through template screening.

Matthews TP, Klair S, Burns S, Boxall K, Cherry M, Fisher M, Westwood IM, Walton MI, McHardy T, Cheung KM, Van Montfort R, Williams D, Aherne GW, Garrett MD, Reader J, Collins I.

J Med Chem. 2009 Aug 13;52(15):4810-9. doi: 10.1021/jm900314j.

PMID:
19572549
[PubMed - indexed for MEDLINE]
20.

Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.

Dehnhardt CM, Venkatesan AM, Chen Z, Delos-Santos E, Ayral-Kaloustian S, Brooijmans N, Yu K, Hollander I, Feldberg L, Lucas J, Mallon R.

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4773-8. doi: 10.1016/j.bmcl.2011.06.063. Epub 2011 Jun 21.

PMID:
21763134
[PubMed - indexed for MEDLINE]
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