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1.

Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.

Bardelle C, Cross D, Davenport S, Kettle JG, Ko EJ, Leach AG, Mortlock A, Read J, Roberts NJ, Robins P, Williams EJ.

Bioorg Med Chem Lett. 2008 May 1;18(9):2776-80. doi: 10.1016/j.bmcl.2008.04.015. Epub 2008 Apr 10.

PMID:
18434142
2.

Inhibitors of the tyrosine kinase EphB4. Part 2: structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines.

Bardelle C, Coleman T, Cross D, Davenport S, Kettle JG, Ko EJ, Leach AG, Mortlock A, Read J, Roberts NJ, Robins P, Williams EJ.

Bioorg Med Chem Lett. 2008 Nov 1;18(21):5717-21. doi: 10.1016/j.bmcl.2008.09.087. Epub 2008 Sep 27.

PMID:
18851911
3.

Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series.

Barlaam B, Ducray R, Lambert-van der Brempt C, Plé P, Bardelle C, Brooks N, Coleman T, Cross D, Kettle JG, Read J.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2207-11. doi: 10.1016/j.bmcl.2011.03.009.

PMID:
21441027
4.

Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4).

Lafleur K, Huang D, Zhou T, Caflisch A, Nevado C.

J Med Chem. 2009 Oct 22;52(20):6433-46. doi: 10.1021/jm9009444.

PMID:
19788238
5.

Inhibitors of the tyrosine kinase EphB4. Part 3: identification of non-benzodioxole-based kinase inhibitors.

Bardelle C, Barlaam B, Brooks N, Coleman T, Cross D, Ducray R, Green I, Brempt CL, Olivier A, Read J.

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6242-5. doi: 10.1016/j.bmcl.2010.08.100. Epub 2010 Sep 16.

PMID:
20850301
6.

Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies.

Liu M, Wang S, Clampit JE, Gum RJ, Haasch DL, Rondinone CM, Trevillyan JM, Abad-Zapatero C, Fry EH, Sham HL, Liu G.

Bioorg Med Chem Lett. 2007 Feb 1;17(3):668-72. Epub 2006 Nov 2.

PMID:
17107797
7.

Structure-based tailoring of compound libraries for high-throughput screening: discovery of novel EphB4 kinase inhibitors.

Kolb P, Kipouros CB, Huang D, Caflisch A.

Proteins. 2008 Oct;73(1):11-8. doi: 10.1002/prot.22028.

PMID:
18384152
8.

Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors.

Waterson AG, Petrov KG, Hornberger KR, Hubbard RD, Sammond DM, Smith SC, Dickson HD, Caferro TR, Hinkle KW, Stevens KL, Dickerson SH, Rusnak DW, Spehar GM, Wood ER, Griffin RJ, Uehling DE.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1332-6. doi: 10.1016/j.bmcl.2009.01.080. Epub 2009 Feb 7.

PMID:
19208477
9.

Novel imidazo[1,2-a]pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: optimization of the aniline.

Ducray R, Jones CD, Jung FH, Simpson I, Curwen J, Pass M.

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4702-4. doi: 10.1016/j.bmcl.2011.06.090. Epub 2011 Jun 25.

PMID:
21764307
10.

Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.

Gracias V, Ji Z, Akritopoulou-Zanze I, Abad-Zapatero C, Huth JR, Song D, Hajduk PJ, Johnson EF, Glaser KB, Marcotte PA, Pease L, Soni NB, Stewart KD, Davidsen SK, Michaelides MR, Djuric SW.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2691-5. doi: 10.1016/j.bmcl.2008.03.021. Epub 2008 Mar 10.

PMID:
18362070
11.

Discovery and in vitro evaluation of potent kinase inhibitors: Pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines.

Alberti MJ, Auten EP, Lackey KE, McDonald OB, Wood ER, Preugschat F, Cutler GJ, Kane-Carson L, Liu W, Jung DK.

Bioorg Med Chem Lett. 2005 Aug 15;15(16):3778-81.

PMID:
15993060
12.

Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable.

Buttar D, Edge M, Emery SC, Fitzek M, Forder C, Griffen A, Hayter B, Hayward CF, Hopcroft PJ, Luke RW, Page K, Stawpert J, Wright A.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4723-6. doi: 10.1016/j.bmcl.2008.06.106. Epub 2008 Jul 23.

PMID:
18676144
13.

Identification of 4-aminopyrazolylpyrimidines as potent inhibitors of Trk kinases.

Wang T, Lamb ML, Scott DA, Wang H, Block MH, Lyne PD, Lee JW, Davies AM, Zhang HJ, Zhu Y, Gu F, Han Y, Wang B, Mohr PJ, Kaus RJ, Josey JA, Hoffmann E, Thress K, Macintyre T, Wang H, Omer CA, Yu D.

J Med Chem. 2008 Aug 14;51(15):4672-84. doi: 10.1021/jm800343j. Epub 2008 Jul 23.

PMID:
18646745
14.

Entry into a new class of protein kinase inhibitors by pseudo ring design.

Furet P, Caravatti G, Guagnano V, Lang M, Meyer T, Schoepfer J.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):897-900. doi: 10.1016/j.bmcl.2007.12.041. Epub 2008 Jan 14.

PMID:
18248988
15.

Rational design of 4-amino-5,6-diaryl-furo[2,3-d]pyrimidines as potent glycogen synthase kinase-3 inhibitors.

Miyazaki Y, Maeda Y, Sato H, Nakano M, Mellor GW.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1967-71. doi: 10.1016/j.bmcl.2008.01.113. Epub 2008 Feb 2.

PMID:
18280153
16.

Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors.

Huang H, Hutta DA, Hu H, DesJarlais RL, Schubert C, Petrounia IP, Chaikin MA, Manthey CL, Player MR.

Bioorg Med Chem Lett. 2008 Apr 1;18(7):2355-61. doi: 10.1016/j.bmcl.2008.02.070. Epub 2008 Mar 4.

PMID:
18342505
17.

Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.

Richardson CM, Williamson DS, Parratt MJ, Borgognoni J, Cansfield AD, Dokurno P, Francis GL, Howes R, Moore JD, Murray JB, Robertson A, Surgenor AE, Torrance CJ.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1353-7. Epub 2005 Dec 1.

PMID:
16325401
18.

Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.

Zhang G, Ren P, Gray NS, Sim T, Wang X, Liu Y, Che J, Dong W, Tian SS, Sandberg ML, Spalding TA, Romeo R, Iskandar M, Wang Z, Seidel HM, Karanewsky DS, He Y.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6691-5. doi: 10.1016/j.bmcl.2009.09.123. Epub 2009 Oct 12.

PMID:
19854052
19.

Synthesis and SAR of 2-phenoxypyridines as novel c-Jun N-terminal kinase inhibitors.

Song X, Chen W, Lin L, Ruiz CH, Cameron MD, Duckett DR, Kamenecka TM.

Bioorg Med Chem Lett. 2011 Dec 1;21(23):7072-5. doi: 10.1016/j.bmcl.2011.09.090. Epub 2011 Sep 29.

PMID:
22004719
20.

7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.

Frey RR, Curtin ML, Albert DH, Glaser KB, Pease LJ, Soni NB, Bouska JJ, Reuter D, Stewart KD, Marcotte P, Bukofzer G, Li J, Davidsen SK, Michaelides MR.

J Med Chem. 2008 Jul 10;51(13):3777-87. doi: 10.1021/jm701397k. Epub 2008 Jun 17.

PMID:
18557606
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