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Items: 1 to 20 of 175

1.

Discovery and synthesis of novel 4-aminopyrrolopyrimidine Tie-2 kinase inhibitors for the treatment of solid tumors.

Arcari JT, Beebe JS, Berliner MA, Bernardo V, Boehm M, Borzillo GV, Clark T, Cohen BD, Connell RD, Frost HN, Gordon DA, Hungerford WM, Kakar SM, Kanter A, Keene NF, Knauth EA, Lagreca SD, Lu Y, Martinez-Alsina L, Marx MA, Morris J, Patel NC, Savage D, Soderstrom CI, Thompson C, Tkalcevic G, Tom NJ, Vajdos FF, Valentine JJ, Vincent PW, Wessel MD, Chen JM.

Bioorg Med Chem Lett. 2013 May 15;23(10):3059-63. doi: 10.1016/j.bmcl.2013.03.012. Epub 2013 Mar 21.

PMID:
23566514
2.

Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors.

Brasca MG, Nesi M, Avanzi N, Ballinari D, Bandiera T, Bertrand J, Bindi S, Canevari G, Carenzi D, Casero D, Ceriani L, Ciomei M, Cirla A, Colombo M, Cribioli S, Cristiani C, Della Vedova F, Fachin G, Fasolini M, Felder ER, Galvani A, Isacchi A, Mirizzi D, Motto I, Panzeri A, Pesenti E, Vianello P, Gnocchi P, Donati D.

Bioorg Med Chem. 2014 Sep 1;22(17):4998-5012. doi: 10.1016/j.bmc.2014.06.025. Epub 2014 Jun 21.

PMID:
25009002
3.

Discovery of pyrrolopyrimidine inhibitors of Akt.

Blake JF, Kallan NC, Xiao D, Xu R, Bencsik JR, Skelton NJ, Spencer KL, Mitchell IS, Woessner RD, Gloor SL, Risom T, Gross SD, Martinson M, Morales TH, Vigers GP, Brandhuber BJ.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5607-12. doi: 10.1016/j.bmcl.2010.08.053. Epub 2010 Aug 13.

PMID:
20810279
4.

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
5.

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.

Fairhurst RA, Marsilje TH, Stutz S, Boos A, Niklaus M, Chen B, Jiang S, Lu W, Furet P, McCarthy C, Stauffer F, Guagnano V, Vaupel A, Michellys PY, Schnell C, Jeay S.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):2057-64. doi: 10.1016/j.bmcl.2016.02.075. Epub 2016 Feb 26.

PMID:
26951753
6.

Structure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors.

Le Brazidec JY, Pasis A, Tam B, Boykin C, Wang D, Marcotte DJ, Claassen G, Chong JH, Chao J, Fan J, Nguyen K, Silvian L, Ling L, Zhang L, Choi M, Teng M, Pathan N, Zhao S, Li T, Taveras A.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):4033-7. doi: 10.1016/j.bmcl.2012.04.085. Epub 2012 Apr 25.

PMID:
22607669
7.

Synthesis and structure based optimization of novel Akt inhibitors.

Lippa B, Pan G, Corbett M, Li C, Kauffman GS, Pandit J, Robinson S, Wei L, Kozina E, Marr ES, Borzillo G, Knauth E, Barbacci-Tobin EG, Vincent P, Troutman M, Baker D, Rajamohan F, Kakar S, Clark T, Morris J.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3359-63. doi: 10.1016/j.bmcl.2008.04.034. Epub 2008 Apr 15.

PMID:
18456494
8.

Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agents.

Gangjee A, Namjoshi OA, Yu J, Ihnat MA, Thorpe JE, Warnke LA.

Bioorg Med Chem. 2008 May 15;16(10):5514-28. doi: 10.1016/j.bmc.2008.04.019. Epub 2008 Apr 14.

9.

Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I).

Zhang L, Fan J, Chong JH, Cesena A, Tam BY, Gilson C, Boykin C, Wang D, Aivazian D, Marcotte D, Xiao G, Le Brazidec JY, Piao J, Lundgren K, Hong K, Vu K, Nguyen K, Gan LS, Silvian L, Ling L, Teng M, Reff M, Takeda N, Timple N, Wang Q, Morena R, Khan S, Zhao S, Li T, Lee WC, Taveras AG, Chao J.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5633-7. doi: 10.1016/j.bmcl.2011.06.129. Epub 2011 Jul 13.

PMID:
21798738
10.

Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases.

Addie M, Ballard P, Buttar D, Crafter C, Currie G, Davies BR, Debreczeni J, Dry H, Dudley P, Greenwood R, Johnson PD, Kettle JG, Lane C, Lamont G, Leach A, Luke RW, Morris J, Ogilvie D, Page K, Pass M, Pearson S, Ruston L.

J Med Chem. 2013 Mar 14;56(5):2059-73. doi: 10.1021/jm301762v. Epub 2013 Feb 26.

PMID:
23394218
11.

Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.

Shallal HM, Russu WA.

Eur J Med Chem. 2011 Jun;46(6):2043-57. doi: 10.1016/j.ejmech.2011.02.057. Epub 2011 Mar 3.

PMID:
21429632
12.

Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine derivatives: novel VEGFR2 kinase inhibitors binding to inactive kinase conformation.

Oguro Y, Miyamoto N, Okada K, Takagi T, Iwata H, Awazu Y, Miki H, Hori A, Kamiyama K, Imamura S.

Bioorg Med Chem. 2010 Oct 15;18(20):7260-73. doi: 10.1016/j.bmc.2010.08.017. Epub 2010 Aug 13.

PMID:
20833055
13.

Novel thienopyrimidine and thiazolopyrimidine kinase inhibitors with activity against Tie-2 in vitro and in vivo.

Luke RW, Ballard P, Buttar D, Campbell L, Curwen J, Emery SC, Griffen AM, Hassall L, Hayter BR, Jones CD, McCoull W, Mellor M, Swain ML, Tucker JA.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6670-4. doi: 10.1016/j.bmcl.2009.10.001. Epub 2009 Oct 13.

PMID:
19854647
14.

Synthesis and biological activities of 4-substituted pyrrolo[2,3-a]carbazole Pim kinase inhibitors.

Giraud F, Akué-Gédu R, Nauton L, Candelon N, Debiton E, Théry V, Anizon F, Moreau P.

Eur J Med Chem. 2012 Oct;56:225-36. doi: 10.1016/j.ejmech.2012.08.029. Epub 2012 Aug 30.

PMID:
22982527
15.

Discovery of novel substituted benzo-anellated 4-benzylamino pyrrolopyrimidines as dual EGFR and VEGFR2 inhibitors.

Fischer T, Krüger T, Najjar A, Totzke F, Schächtele C, Sippl W, Ritter C, Hilgeroth A.

Bioorg Med Chem Lett. 2017 Jun 15;27(12):2708-2712. doi: 10.1016/j.bmcl.2017.04.053. Epub 2017 Apr 19.

PMID:
28478927
16.

CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers.

Cheng M, Quail MR, Gingrich DE, Ott GR, Lu L, Wan W, Albom MS, Angeles TS, Aimone LD, Cristofani F, Machiorlatti R, Abele C, Ator MA, Dorsey BD, Inghirami G, Ruggeri BA.

Mol Cancer Ther. 2012 Mar;11(3):670-9. doi: 10.1158/1535-7163.MCT-11-0776. Epub 2011 Dec 27.

17.

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
18.

Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors.

Hu S, Xie G, Zhang DX, Davis C, Long W, Hu Y, Wang F, Kang X, Tan F, Ding L, Wang Y.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6301-5. doi: 10.1016/j.bmcl.2012.06.067. Epub 2012 Jun 28.

PMID:
22959248
19.

Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent.

Li HY, McMillen WT, Heap CR, McCann DJ, Yan L, Campbell RM, Mundla SR, King CH, Dierks EA, Anderson BD, Britt KS, Huss KL, Voss MD, Wang Y, Clawson DK, Yingling JM, Sawyer JS.

J Med Chem. 2008 Apr 10;51(7):2302-6. doi: 10.1021/jm701199p. Epub 2008 Mar 4.

PMID:
18314943
20.

SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.

Forsyth T, Kearney PC, Kim BG, Johnson HW, Aay N, Arcalas A, Brown DS, Chan V, Chen J, Du H, Epshteyn S, Galan AA, Huynh TP, Ibrahim MA, Kane B, Koltun ES, Mann G, Meyr LE, Lee MS, Lewis GL, Noguchi RT, Pack M, Ridgway BH, Shi X, Takeuchi CS, Zu P, Leahy JW, Nuss JM, Aoyama R, Engst S, Gendreau SB, Kassees R, Li J, Lin SH, Martini JF, Stout T, Tong P, Woolfrey J, Zhang W, Yu P.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7653-8. doi: 10.1016/j.bmcl.2012.10.007. Epub 2012 Oct 16.

PMID:
23127890

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