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Items: 1 to 20 of 206

1.

Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).

Burns CJ, Bourke DG, Andrau L, Bu X, Charman SA, Donohue AC, Fantino E, Farrugia M, Feutrill JT, Joffe M, Kling MR, Kurek M, Nero TL, Nguyen T, Palmer JT, Phillips I, Shackleford DM, Sikanyika H, Styles M, Su S, Treutlein H, Zeng J, Wilks AF.

Bioorg Med Chem Lett. 2009 Oct 15;19(20):5887-92. doi: 10.1016/j.bmcl.2009.08.071. Epub 2009 Aug 23.

PMID:
19762238
2.

Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.

Berger DM, Torres N, Dutia M, Powell D, Ciszewski G, Gopalsamy A, Levin JI, Kim KH, Xu W, Wilhelm J, Hu Y, Collins K, Feldberg L, Kim S, Frommer E, Wojciechowicz D, Mallon R.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6519-23. doi: 10.1016/j.bmcl.2009.10.049. Epub 2009 Oct 26.

PMID:
19864136
3.

2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.

Ledeboer MW, Pierce AC, Duffy JP, Gao H, Messersmith D, Salituro FG, Nanthakumar S, Come J, Zuccola HJ, Swenson L, Shlyakter D, Mahajan S, Hoock T, Fan B, Tsai WJ, Kolaczkowski E, Carrier S, Hogan JK, Zessis R, Pazhanisamy S, Bennani YL.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6529-33. doi: 10.1016/j.bmcl.2009.10.053. Epub 2009 Oct 24.

PMID:
19857967
4.

Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.

Malerich JP, Lam JS, Hart B, Fine RM, Klebansky B, Tanga MJ, D'Andrea A.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7454-7. doi: 10.1016/j.bmcl.2010.10.026. Epub 2010 Oct 13.

PMID:
21106455
5.

2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.

Harris CM, Ericsson AM, Argiriadi MA, Barberis C, Borhani DW, Burchat A, Calderwood DJ, Cunha GA, Dixon RW, Frank KE, Johnson EF, Kamens J, Kwak S, Li B, Mullen KD, Perron DC, Wang L, Wishart N, Wu X, Zhang X, Zmetra TR, Talanian RV.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):334-7. doi: 10.1016/j.bmcl.2009.10.103. Epub 2009 Oct 29.

PMID:
19926477
6.

2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.

Gerspacher M, Furet P, Pissot-Soldermann C, Gaul C, Holzer P, Vangrevelinghe E, Lang M, Erdmann D, Radimerski T, Regnier CH, Chene P, De Pover A, Hofmann F, Baffert F, Buhl T, Aichholz R, Blasco F, Endres R, Trappe J, Drueckes P.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1724-7. doi: 10.1016/j.bmcl.2010.01.069. Epub 2010 Jan 21.

PMID:
20138510
7.

Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.

Wang T, Duffy JP, Wang J, Halas S, Salituro FG, Pierce AC, Zuccola HJ, Black JR, Hogan JK, Jepson S, Shlyakter D, Mahajan S, Gu Y, Hoock T, Wood M, Furey BF, Frantz JD, Dauffenbach LM, Germann UA, Fan B, Namchuk M, Bennani YL, Ledeboer MW.

J Med Chem. 2009 Dec 24;52(24):7938-41. doi: 10.1021/jm901383u.

PMID:
20014869
8.

A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors.

Wang T, Ledeboer MW, Duffy JP, Salituro FG, Pierce AC, Zuccola HJ, Block E, Shlyakter D, Hogan JK, Bennani YL.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):153-6. doi: 10.1016/j.bmcl.2009.11.021. Epub 2009 Nov 12. Erratum in: Bioorg Med Chem Lett. 2010 Apr 15;20(8):2684. Salituro, Francesco G [added].

PMID:
19945871
9.

Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.

Wurz RP, Pettus LH, Henkle B, Sherman L, Plant M, Miner K, McBride HJ, Wong LM, Saris CJ, Lee MR, Chmait S, Mohr C, Hsieh F, Tasker AS.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1680-4. doi: 10.1016/j.bmcl.2010.01.059. Epub 2010 Jan 21.

PMID:
20138761
10.

Triazine and pyrimidine based ROCK inhibitors with efficacy in spontaneous hypertensive rat model.

Ho KK, Beasley JR, Belanger L, Black D, Chan JH, Dunn D, Hu B, Klon A, Kultgen SG, Ohlmeyer M, Parlato SM, Ray PC, Pham Q, Rong Y, Roughton AL, Walker TL, Wright J, Xu K, Xu Y, Zhang L, Webb M.

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6027-31. doi: 10.1016/j.bmcl.2009.09.046. Epub 2009 Sep 17.

PMID:
19800787
11.

Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.

Hanan EJ, van Abbema A, Barrett K, Blair WS, Blaney J, Chang C, Eigenbrot C, Flynn S, Gibbons P, Hurley CA, Kenny JR, Kulagowski J, Lee L, Magnuson SR, Morris C, Murray J, Pastor RM, Rawson T, Siu M, Ultsch M, Zhou A, Sampath D, Lyssikatos JP.

J Med Chem. 2012 Nov 26;55(22):10090-107. doi: 10.1021/jm3012239. Epub 2012 Oct 24.

PMID:
23061660
12.

Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors.

Asaki T, Sugiyama Y, Hamamoto T, Higashioka M, Umehara M, Naito H, Niwa T.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1421-5. Epub 2005 Dec 5.

PMID:
16332440
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.

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
15.

Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.

Labadie S, Barrett K, Blair WS, Chang C, Deshmukh G, Eigenbrot C, Gibbons P, Johnson A, Kenny JR, Kohli PB, Liimatta M, Lupardus PJ, Shia S, Steffek M, Ubhayakar S, van Abbema A, Zak M.

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5923-30. doi: 10.1016/j.bmcl.2013.08.082. Epub 2013 Aug 27.

PMID:
24042009
16.

Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors.

Liang X, Huang Y, Zang J, Gao Q, Wang B, Xu W, Zhang Y.

Bioorg Med Chem. 2016 Jun 15;24(12):2660-72. doi: 10.1016/j.bmc.2016.04.030. Epub 2016 Apr 20.

PMID:
27137359
17.

Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1).

Huang S, Li R, Connolly PJ, Emanuel S, Fuentes-Pesquera A, Adams M, Gruninger RH, Seraj J, Middleton SA, Davis JM, Moffat DF.

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2179-83. Epub 2007 Feb 2.

PMID:
17317182
18.

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
19.

Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors.

Ioannidis S, Lamb ML, Davies AM, Almeida L, Su M, Bebernitz G, Ye M, Bell K, Alimzhanov M, Zinda M.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6524-8. doi: 10.1016/j.bmcl.2009.10.054. Epub 2009 Oct 24.

PMID:
19857966
20.

2,4-Diaminopyrimidine MK2 inhibitors. Part I: Observation of an unexpected inhibitor binding mode.

Argiriadi MA, Ericsson AM, Harris CM, Banach DL, Borhani DW, Calderwood DJ, Demers MD, Dimauro J, Dixon RW, Hardman J, Kwak S, Li B, Mankovich JA, Marcotte D, Mullen KD, Ni B, Pietras M, Sadhukhan R, Sousa S, Tomlinson MJ, Wang L, Xiang T, Talanian RV.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):330-3. doi: 10.1016/j.bmcl.2009.10.102. Epub 2009 Oct 29.

PMID:
19919896

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