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Items: 1 to 20 of 149

1.

Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.

Meng Z, Ciavarri JP, McRiner A, Zhao Y, Zhao L, Reddy PA, Zhang X, Fischmann TO, Whitehurst C, Arshad Siddiqui M.

Bioorg Med Chem Lett. 2013 May 15;23(10):2863-7. doi: 10.1016/j.bmcl.2013.03.100. Epub 2013 Apr 4.

PMID:
23587425
2.

Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.

Belanger DB, Curran PJ, Hruza A, Voigt J, Meng Z, Mandal AK, Siddiqui MA, Basso AD, Gray K.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5170-4. doi: 10.1016/j.bmcl.2010.07.008. Epub 2010 Jul 8.

PMID:
20674350
3.

Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.

Robarge KD, Lee W, Eigenbrot C, Ultsch M, Wiesmann C, Heald R, Price S, Hewitt J, Jackson P, Savy P, Burton B, Choo EF, Pang J, Boggs J, Yang A, Yang X, Baumgardner M.

Bioorg Med Chem Lett. 2014 Oct 1;24(19):4714-23. doi: 10.1016/j.bmcl.2014.08.008. Epub 2014 Aug 15.

PMID:
25193232
4.

Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors.

Zeng H, Belanger DB, Curran PJ, Shipps GW Jr, Miao H, Bracken JB, Arshad Siddiqui M, Malkowski M, Wang Y.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5870-5. doi: 10.1016/j.bmcl.2011.07.101. Epub 2011 Aug 3.

PMID:
21855335
5.

Bioisosteric approach to the discovery of imidazo[1,2-a]pyrazines as potent Aurora kinase inhibitors.

Meng Z, Kulkarni BA, Kerekes AD, Mandal AK, Esposite SJ, Belanger DB, Reddy PA, Basso AD, Tevar S, Gray K, Jones J, Smith EB, Doll RJ, Siddiqui MA.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):592-8. doi: 10.1016/j.bmcl.2010.10.008. Epub 2010 Oct 12.

PMID:
21075632
6.

Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.

Bouloc N, Large JM, Kosmopoulou M, Sun C, Faisal A, Matteucci M, Reynisson J, Brown N, Atrash B, Blagg J, McDonald E, Linardopoulos S, Bayliss R, Bavetsias V.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):5988-93. doi: 10.1016/j.bmcl.2010.08.091. Epub 2010 Aug 21.

PMID:
20833547
7.

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
8.

Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.

Belanger DB, Williams MJ, Curran PJ, Mandal AK, Meng Z, Rainka MP, Yu T, Shih NY, Siddiqui MA, Liu M, Tevar S, Lee S, Liang L, Gray K, Yaremko B, Jones J, Smith EB, Prelusky DB, Basso AD.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6739-43. doi: 10.1016/j.bmcl.2010.08.140. Epub 2010 Sep 18.

PMID:
20855207
9.

Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors.

Tardy S, Orsato A, Mologni L, Bisson WH, Donadoni C, Gambacorti-Passerini C, Scapozza L, Gueyrard D, Goekjian PG.

Bioorg Med Chem. 2014 Feb 15;22(4):1303-12. doi: 10.1016/j.bmc.2014.01.007. Epub 2014 Jan 10.

PMID:
24468632
10.

Discovery of potent, selective and orally bioavailable imidazo[1,5-a]pyrazine derived ACK1 inhibitors.

Jin M, Wang J, Kleinberg A, Kadalbajoo M, Siu KW, Cooke A, Bittner MA, Yao Y, Thelemann A, Ji Q, Bhagwat S, Mulvihill KM, Rechka JA, Pachter JA, Crew AP, Epstein D, Mulvihill MJ.

Bioorg Med Chem Lett. 2013 Feb 15;23(4):979-84. doi: 10.1016/j.bmcl.2012.12.042. Epub 2012 Dec 21.

PMID:
23317569
11.

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
12.

Theoretical analysis of the binding of potential inhibitors to protein kinases MK2 and MK3.

Araújo PM, da Silva LP, Esteves da Silva JC.

Med Chem. 2015;11(6):573-9.

PMID:
25665652
13.

Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 1.

Dwyer MP, Paruch K, Labroli M, Alvarez C, Keertikar KM, Poker C, Rossman R, Fischmann TO, Duca JS, Madison V, Parry D, Davis N, Seghezzi W, Wiswell D, Guzi TJ.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):467-70. doi: 10.1016/j.bmcl.2010.10.113. Epub 2010 Oct 27.

PMID:
21094608
14.

Design of granulatimide and isogranulatimide analogues as potential Chk1 inhibitors: Study of amino-platforms for their synthesis.

Lavrard H, Rodriguez F, Delfourne E.

Bioorg Med Chem. 2014 Sep 1;22(17):4961-7. doi: 10.1016/j.bmc.2014.06.028. Epub 2014 Jun 30.

PMID:
25047935
15.

Discovery of 5-(2-(phenylamino)pyrimidin-4-yl)thiazol-2(3H)-one derivatives as potent Mnk2 inhibitors: synthesis, SAR analysis and biological evaluation.

Diab S, Teo T, Kumarasiri M, Li P, Yu M, Lam F, Basnet SK, Sykes MJ, Albrecht H, Milne R, Wang S.

ChemMedChem. 2014 May;9(5):962-72. doi: 10.1002/cmdc.201300552. Epub 2014 Feb 12.

PMID:
24677692
16.

Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 2.

Labroli M, Paruch K, Dwyer MP, Alvarez C, Keertikar K, Poker C, Rossman R, Duca JS, Fischmann TO, Madison V, Parry D, Davis N, Seghezzi W, Wiswell D, Guzi TJ.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):471-4. doi: 10.1016/j.bmcl.2010.10.114. Epub 2010 Oct 28.

PMID:
21094607
17.

Inhibiting NF-κB-inducing kinase (NIK): discovery, structure-based design, synthesis, structure-activity relationship, and co-crystal structures.

Li K, McGee LR, Fisher B, Sudom A, Liu J, Rubenstein SM, Anwer MK, Cushing TD, Shin Y, Ayres M, Lee F, Eksterowicz J, Faulder P, Waszkowycz B, Plotnikova O, Farrelly E, Xiao SH, Chen G, Wang Z.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1238-44. doi: 10.1016/j.bmcl.2013.01.012. Epub 2013 Jan 11.

PMID:
23374866
18.

Structure-activity relationship studies of imidazo[1,2-c]pyrimidine derivatives as potent and orally effective Syk family kinases inhibitors.

Hirabayashi A, Mukaiyama H, Kobayashi H, Shiohara H, Nakayama S, Ozawa M, Tsuji E, Miyazawa K, Misawa K, Ohnota H, Isaji M.

Bioorg Med Chem. 2008 Oct 15;16(20):9247-60. doi: 10.1016/j.bmc.2008.09.015. Epub 2008 Sep 9.

PMID:
18823784
19.

Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.

Xiao D, Zhu X, Sofolarides M, Degrado S, Shao N, Rao A, Chen X, Aslanian R, Fossetta J, Tian F, Trivedi P, Lundell D, Palani A.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3609-13. doi: 10.1016/j.bmcl.2014.05.024. Epub 2014 May 16.

PMID:
24913714
20.

Discovery of selective 4-Amino-pyridopyrimidine inhibitors of MAP4K4 using fragment-based lead identification and optimization.

Crawford TD, Ndubaku CO, Chen H, Boggs JW, Bravo BJ, Delatorre K, Giannetti AM, Gould SE, Harris SF, Magnuson SR, McNamara E, Murray LJ, Nonomiya J, Sambrone A, Schmidt S, Smyczek T, Stanley M, Vitorino P, Wang L, West K, Wu P, Ye W.

J Med Chem. 2014 Apr 24;57(8):3484-93. doi: 10.1021/jm500155b. Epub 2014 Apr 9.

PMID:
24673130

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