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Items: 1 to 20 of 179

1.

The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing.

Jones CD, Andrews DM, Barker AJ, Blades K, Daunt P, East S, Geh C, Graham MA, Johnson KM, Loddick SA, McFarland HM, McGregor A, Moss L, Rudge DA, Simpson PB, Swain ML, Tam KY, Tucker JA, Walker M.

Bioorg Med Chem Lett. 2008 Dec 15;18(24):6369-73. doi: 10.1016/j.bmcl.2008.10.102. Epub 2008 Oct 25.

PMID:
18996007
2.

Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors.

Jones CD, Andrews DM, Barker AJ, Blades K, Byth KF, Finlay MR, Geh C, Green CP, Johannsen M, Walker M, Weir HM.

Bioorg Med Chem Lett. 2008 Dec 15;18(24):6486-9. doi: 10.1016/j.bmcl.2008.10.075. Epub 2008 Oct 22.

PMID:
18986805
3.

Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors.

Dwyer MP, Paruch K, Alvarez C, Doll RJ, Keertikar K, Duca J, Fischmann TO, Hruza A, Madison V, Lees E, Parry D, Seghezzi W, Sgambellone N, Shanahan F, Wiswell D, Guzi TJ.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6216-9. Epub 2007 Sep 8.

PMID:
17904366
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.

Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation.

DiMauro EF, Newcomb J, Nunes JJ, Bemis JE, Boucher C, Chai L, Chaffee SC, Deak HL, Epstein LF, Faust T, Gallant P, Gore A, Gu Y, Henkle B, Hsieh F, Huang X, Kim JL, Lee JH, Martin MW, McGowan DC, Metz D, Mohn D, Morgenstern KA, Oliveira-dos-Santos A, Patel VF, Powers D, Rose PE, Schneider S, Tomlinson SA, Tudor YY, Turci SM, Welcher AA, Zhao H, Zhu L, Zhu X.

J Med Chem. 2008 Mar 27;51(6):1681-94. doi: 10.1021/jm7010996. Epub 2008 Mar 6.

PMID:
18321037
6.

Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors.

Meng W, Brigance RP, Chao HJ, Fura A, Harrity T, Marcinkeviciene J, O'Connor SP, Tamura JK, Xie D, Zhang Y, Klei HE, Kish K, Weigelt CA, Turdi H, Wang A, Zahler R, Kirby MS, Hamann LG.

J Med Chem. 2010 Aug 12;53(15):5620-8. doi: 10.1021/jm100634a.

PMID:
20684603
7.

Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines.

Lee J, Kim H, Yu H, Chung JY, Oh CH, Yoo KH, Sim T, Hah JM.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1573-7. doi: 10.1016/j.bmcl.2010.01.064. Epub 2010 Jan 21.

PMID:
20149658
8.

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
9.

Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors.

Anderson M, Andrews DM, Barker AJ, Brassington CA, Breed J, Byth KF, Culshaw JD, Finlay MR, Fisher E, McMiken HH, Green CP, Heaton DW, Nash IA, Newcombe NJ, Oakes SE, Pauptit RA, Roberts A, Stanway JJ, Thomas AP, Tucker JA, Walker M, Weir HM.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5487-92. doi: 10.1016/j.bmcl.2008.09.024. Epub 2008 Sep 10.

PMID:
18815031
10.

Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.

Das J, Moquin RV, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly K, Doweyko AM, Sack JS, Zhang H, Kiefer SE, Kish K, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2652-7. doi: 10.1016/j.bmcl.2008.03.019. Epub 2008 Mar 10.

PMID:
18359226
11.

Amide-based inhibitors of p38alpha MAP kinase. Part 1: discovery of novel N-pyridyl amide lead molecules.

Luedtke GR, Schinzel K, Tan X, Tester RW, Nashashibi I, Xu YJ, Dugar S, Levy DE, Jung J.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2556-9. doi: 10.1016/j.bmcl.2010.02.088. Epub 2010 Mar 10.

PMID:
20346653
12.

Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).

Farmer LJ, Bemis G, Britt SD, Cochran J, Connors M, Harrington EM, Hoock T, Markland W, Nanthakumar S, Taslimi P, Ter Haar E, Wang J, Zhaveri D, Salituro FG.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6231-5. doi: 10.1016/j.bmcl.2008.09.106. Epub 2008 Oct 7.

PMID:
18938080
13.

Structure-based design of PDK1 inhibitors.

Poulsen A, Blanchard S, Soh CK, Lee C, Williams M, Wang H, Dymock B.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):305-7. doi: 10.1016/j.bmcl.2011.11.006. Epub 2011 Nov 9.

PMID:
22119465
14.

A phase I pharmacodynamic study of the effects of the cyclin-dependent kinase-inhibitor AZD5438 on cell cycle markers within the buccal mucosa, plucked scalp hairs and peripheral blood mononucleocytes of healthy male volunteers.

Camidge DR, Pemberton M, Growcott J, Amakye D, Wilson D, Swaisland H, Forder C, Wilkinson R, Byth K, Hughes A.

Cancer Chemother Pharmacol. 2007 Sep;60(4):479-88. Epub 2006 Dec 2.

PMID:
17143601
15.

Macrocyclic aminopyrimidines as multitarget CDK and VEGF-R inhibitors with potent antiproliferative activities.

Lücking U, Siemeister G, Schäfer M, Briem H, Krüger M, Lienau P, Jautelat R.

ChemMedChem. 2007 Jan;2(1):63-77.

PMID:
17131463
16.

Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38alpha mitogen-activated protein kinase.

Kim DK, Lim JH, Lee JA, Dewang PM.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4006-10. doi: 10.1016/j.bmcl.2008.06.007. Epub 2008 Jun 6.

PMID:
18571921
17.

Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of Cyclin D1-CDK4: synthesis, biological evaluation, and structure-activity relationships.

Horiuchi T, Chiba J, Uoto K, Soga T.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):305-8. doi: 10.1016/j.bmcl.2008.11.090. Epub 2008 Nov 27.

PMID:
19091560
18.

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
19.

Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.

Brasca MG, Albanese C, Alzani R, Amici R, Avanzi N, Ballinari D, Bischoff J, Borghi D, Casale E, Croci V, Fiorentini F, Isacchi A, Mercurio C, Nesi M, Orsini P, Pastori W, Pesenti E, Pevarello P, Roussel P, Varasi M, Volpi D, Vulpetti A, Ciomei M.

Bioorg Med Chem. 2010 Mar 1;18(5):1844-53. doi: 10.1016/j.bmc.2010.01.042. Epub 2010 Jan 25.

PMID:
20153204
20.

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
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