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Results: 1 to 20 of 126

1.

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
[PubMed - indexed for MEDLINE]
2.

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
[PubMed - indexed for MEDLINE]
3.

Potent and selective cyclohexyl-derived imidazopyrazine insulin-like growth factor 1 receptor inhibitors with in vivo efficacy.

Jin M, Kleinberg A, Cooke A, Gokhale PC, Foreman K, Dong H, Siu KW, Bittner MA, Mulvihill KM, Yao Y, Landfair D, O'Connor M, Mak G, Pachter JA, Wild R, Rosenfeld-Franklin M, Ji Q, Mulvihill MJ.

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1176-80. doi: 10.1016/j.bmcl.2010.12.094. Epub 2010 Dec 23.

PMID:
21251824
[PubMed - indexed for MEDLINE]
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
[PubMed - indexed for MEDLINE]
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
[PubMed - indexed for MEDLINE]
6.

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
[PubMed - indexed for MEDLINE]
7.

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
[PubMed - indexed for MEDLINE]
8.

Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.

Currie KS, Kropf JE, Lee T, Blomgren P, Xu J, Zhao Z, Gallion S, Whitney JA, Maclin D, Lansdon EB, Maciejewski P, Rossi AM, Rong H, Macaluso J, Barbosa J, Di Paolo JA, Mitchell SA.

J Med Chem. 2014 May 8;57(9):3856-73. doi: 10.1021/jm500228a. Epub 2014 Apr 29.

PMID:
24779514
[PubMed - indexed for MEDLINE]
9.

Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.

Martínez González S, Hernández AI, Varela C, Lorenzo M, Ramos-Lima F, Cendón E, Cebrián D, Aguirre E, Gomez-Casero E, Albarrán MI, Alfonso P, García-Serelde B, Mateos G, Oyarzabal J, Rabal O, Mulero F, Gonzalez-Granda T, Link W, Fominaya J, Barbacid M, Bischoff JR, Pizcueta P, Blanco-Aparicio C, Pastor J.

Bioorg Med Chem Lett. 2012 Aug 15;22(16):5208-14. doi: 10.1016/j.bmcl.2012.06.093. Epub 2012 Jul 4.

PMID:
22819764
[PubMed - indexed for MEDLINE]
10.

Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor.

Martínez González S, Hernández AI, Varela C, Rodríguez-Arístegui S, Lorenzo M, Rodríguez A, Rivero V, Martín JI, Saluste CG, Ramos-Lima F, Cendón E, Cebrián D, Aguirre E, Gomez-Casero E, Albarrán M, Alfonso P, García-Serelde B, Oyarzabal J, Rabal O, Mulero F, Gonzalez-Granda T, Link W, Fominaya J, Barbacid M, Bischoff JR, Pizcueta P, Pastor J.

Bioorg Med Chem Lett. 2012 May 15;22(10):3460-6. doi: 10.1016/j.bmcl.2012.03.090. Epub 2012 Mar 29.

PMID:
22520259
[PubMed - indexed for MEDLINE]
11.

Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.

Mulvihill MJ, Ji QS, Coate HR, Cooke A, Dong H, Feng L, Foreman K, Rosenfeld-Franklin M, Honda A, Mak G, Mulvihill KM, Nigro AI, O'Connor M, Pirrit C, Steinig AG, Siu K, Stolz KM, Sun Y, Tavares PA, Yao Y, Gibson NW.

Bioorg Med Chem. 2008 Feb 1;16(3):1359-75. Epub 2007 Oct 23.

PMID:
17983756
[PubMed - indexed for MEDLINE]
12.

Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.

Milkiewicz KL, Weinberg LR, Albom MS, Angeles TS, Cheng M, Ghose AK, Roemmele RC, Theroff JP, Underiner TL, Zificsak CA, Dorsey BD.

Bioorg Med Chem. 2010 Jun 15;18(12):4351-62. doi: 10.1016/j.bmc.2010.04.087. Epub 2010 Apr 29.

PMID:
20483621
[PubMed - indexed for MEDLINE]
13.

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
[PubMed - indexed for MEDLINE]
14.

Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.

Mitchell SA, Danca MD, Blomgren PA, Darrow JW, Currie KS, Kropf JE, Lee SH, Gallion SL, Xiong JM, Pippin DA, DeSimone RW, Brittelli DR, Eustice DC, Bourret A, Hill-Drzewi M, Maciejewski PM, Elkin LL.

Bioorg Med Chem Lett. 2009 Dec 15;19(24):6991-5. doi: 10.1016/j.bmcl.2009.10.037. Epub 2009 Oct 15.

PMID:
19879134
[PubMed - indexed for MEDLINE]
15.

The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.

Lewis RT, Bode CM, Choquette DM, Potashman M, Romero K, Stellwagen JC, Teffera Y, Moore E, Whittington DA, Chen H, Epstein LF, Emkey R, Andrews PS, Yu VL, Saffran DC, Xu M, Drew A, Merkel P, Szilvassy S, Brake RL.

J Med Chem. 2012 Jul 26;55(14):6523-40. doi: 10.1021/jm3005866. Epub 2012 Jul 10.

PMID:
22734674
[PubMed - indexed for MEDLINE]
16.

Imidazo[1,2-a]pyrazines as novel PI3K inhibitors.

Martínez González S, Hernández AI, Varela C, Rodríguez-Arístegui S, Alvarez RM, García AB, Lorenzo M, Rivero V, Oyarzabal J, Rabal O, Bischoff JR, Albarrán M, Cebriá A, Alfonso P, Link W, Fominaya J, Pastor J.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1874-8. doi: 10.1016/j.bmcl.2012.01.074. Epub 2012 Jan 28.

PMID:
22325943
[PubMed - indexed for MEDLINE]
17.

Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2-ones as potent and selective mTOR kinase inhibitors.

Mortensen DS, Perrin-Ninkovic SM, Harris R, Lee BG, Shevlin G, Hickman M, Khambatta G, Bisonette RR, Fultz KE, Sankar S.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6793-9. doi: 10.1016/j.bmcl.2011.09.035. Epub 2011 Sep 16.

PMID:
21978683
[PubMed - indexed for MEDLINE]
18.

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
[PubMed - indexed for MEDLINE]
19.

Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.

Kerekes AD, Esposite SJ, Doll RJ, Tagat JR, Yu T, Xiao Y, Zhang Y, Prelusky DB, Tevar S, Gray K, Terracina GA, Lee S, Jones J, Liu M, Basso AD, Smith EB.

J Med Chem. 2011 Jan 13;54(1):201-10. doi: 10.1021/jm1010995. Epub 2010 Dec 3.

PMID:
21128646
[PubMed - indexed for MEDLINE]
20.

Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.

Casuscelli F, Ardini E, Avanzi N, Casale E, Cervi G, D'Anello M, Donati D, Faiardi D, Ferguson RD, Fogliatto G, Galvani A, Marsiglio A, Mirizzi DG, Montemartini M, Orrenius C, Papeo G, Piutti C, Salom B, Felder ER.

Bioorg Med Chem. 2013 Dec 1;21(23):7364-80. doi: 10.1016/j.bmc.2013.09.054. Epub 2013 Oct 2.

PMID:
24139169
[PubMed - indexed for MEDLINE]

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