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Items: 1 to 20 of 103

1.

Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology.

Boga SB, Alhassan AB, Cooper AB, Doll R, Shih NY, Shipps G, Deng Y, Zhu H, Nan Y, Sun R, Zhu L, Desai J, Patel M, Muppalla K, Gao X, Wang J, Yao X, Kelly J, Gudipati S, Paliwal S, Tsui HC, Wang T, Sherborne B, Xiao L, Hruza A, Buevich A, Zhang LK, Hesk D, Samatar AA, Carr D, Long B, Black S, Dayananth P, Windsor W, Kirschmeier P, Bishop R.

Bioorg Med Chem Lett. 2018 Jun 15;28(11):2029-2034. doi: 10.1016/j.bmcl.2018.04.063. Epub 2018 Apr 26.

PMID:
29748051
2.

Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.

Blake JF, Burkard M, Chan J, Chen H, Chou KJ, Diaz D, Dudley DA, Gaudino JJ, Gould SE, Grina J, Hunsaker T, Liu L, Martinson M, Moreno D, Mueller L, Orr C, Pacheco P, Qin A, Rasor K, Ren L, Robarge K, Shahidi-Latham S, Stults J, Sullivan F, Wang W, Yin J, Zhou A, Belvin M, Merchant M, Moffat J, Schwarz JB.

J Med Chem. 2016 Jun 23;59(12):5650-60. doi: 10.1021/acs.jmedchem.6b00389. Epub 2016 Jun 7.

PMID:
27227380
3.

Design and synthesis of potent 1,2,4-trisubstituted imidazolinone derivatives with dual p38αMAPK and ERK1/2 inhibitory activity.

Awadallah FM, Abou-Seri SM, Abdulla MM, Georgey HH.

Eur J Med Chem. 2015 Apr 13;94:397-404. doi: 10.1016/j.ejmech.2015.03.008. Epub 2015 Mar 5.

PMID:
25778995
4.

Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.

Ren L, Grina J, Moreno D, Blake JF, Gaudino JJ, Garrey R, Metcalf AT, Burkard M, Martinson M, Rasor K, Chen H, Dean B, Gould SE, Pacheco P, Shahidi-Latham S, Yin J, West K, Wang W, Moffat JG, Schwarz JB.

J Med Chem. 2015 Feb 26;58(4):1976-91. doi: 10.1021/jm501921k. Epub 2015 Feb 11.

PMID:
25603482
5.

Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2).

Li L, Liu F, Jin N, Tang S, Chen Z, Yang X, Ding J, Geng M, Jiang L, Huang M, Cao J.

Bioorg Med Chem Lett. 2016 Jun 1;26(11):2600-4. doi: 10.1016/j.bmcl.2016.04.029. Epub 2016 Apr 12.

PMID:
27106711
6.

Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells.

Defaux J, Antoine M, Logé C, Le Borgne M, Schuster T, Seipelt I, Aicher B, Teifel M, Günther E, Gerlach M, Marchand P.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3748-52. doi: 10.1016/j.bmcl.2014.06.078. Epub 2014 Jul 3.

PMID:
25022204
7.

Synthesis and antitumor activity of novel 6,7,8-trimethoxy N-aryl-substituted-4-aminoquinazoline derivatives.

Liu F, Huai Z, Xia G, Song L, Li S, Xu Y, Hong K, Yao M, Liu G, Huang Y.

Bioorg Med Chem Lett. 2018 Aug 1;28(14):2561-2565. doi: 10.1016/j.bmcl.2018.05.033. Epub 2018 May 18.

PMID:
29903662
8.

Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.

Deng Y, Shipps GW Jr, Cooper A, English JM, Annis DA, Carr D, Nan Y, Wang T, Zhu HY, Chuang CC, Dayananth P, Hruza AW, Xiao L, Jin W, Kirschmeier P, Windsor WT, Samatar AA.

J Med Chem. 2014 Nov 13;57(21):8817-26. doi: 10.1021/jm500847m. Epub 2014 Oct 22.

PMID:
25313996
9.

Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers.

Lim J, Kelley EH, Methot JL, Zhou H, Petrocchi A, Chen H, Hill SE, Hinton MC, Hruza A, Jung JO, Maclean JK, Mansueto M, Naumov GN, Philippar U, Raut S, Spacciapoli P, Sun D, Siliphaivanh P.

J Med Chem. 2016 Jul 14;59(13):6501-11. doi: 10.1021/acs.jmedchem.6b00708. Epub 2016 Jul 1.

PMID:
27329786
10.

Pyrrolidino Analogues of Gefitinib with Improved EGFR Inhibition, Cancer Cell Cytotoxicity, and Pharmacokinetic Properties.

Fang JK, Xu Z, Zhang Y, Zhang W, Liu B, Fang Y, Sun T.

Anticancer Agents Med Chem. 2016;16(12):1665-1672.

PMID:
27349449
11.

Discovery and evaluation of 3,5-disubstituted indole derivatives as Pim kinase inhibitors.

More KN, Hong VS, Lee A, Park J, Kim S, Lee J.

Bioorg Med Chem Lett. 2018 Aug 1;28(14):2513-2517. doi: 10.1016/j.bmcl.2018.05.054. Epub 2018 May 29.

PMID:
29871845
12.

Synthesis and anticancer activities of 4-(4-substituted piperazin)-5,6,7-trialkoxy quinazoline derivatives.

Zhang Y, Huang YJ, Xiang HM, Wang PY, Hu DY, Xue W, Song BA, Yang S.

Eur J Med Chem. 2014 May 6;78:23-34. doi: 10.1016/j.ejmech.2014.03.036. Epub 2014 Mar 13.

PMID:
24675177
13.

Characterization of a highly selective inhibitor of the Aurora kinases.

Ferguson FM, Doctor ZM, Chaikuad A, Sim T, Kim ND, Knapp S, Gray NS.

Bioorg Med Chem Lett. 2017 Sep 15;27(18):4405-4408. doi: 10.1016/j.bmcl.2017.08.016. Epub 2017 Aug 10.

PMID:
28818446
14.

Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.

Bosanac T, Hickey ER, Ginn J, Kashem M, Kerr S, Kugler S, Li X, Olague A, Schlyer S, Young ER.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3746-9. doi: 10.1016/j.bmcl.2010.04.069. Epub 2010 Apr 21.

PMID:
20471253
15.

Characterization of ERK docking domain inhibitors that induce apoptosis by targeting Rsk-1 and caspase-9.

Boston SR, Deshmukh R, Strome S, Priyakumar UD, MacKerell AD Jr, Shapiro P.

BMC Cancer. 2011 Jan 10;11:7. doi: 10.1186/1471-2407-11-7.

16.

Exploration of N-(2-aminoethyl)piperidine-4-carboxamide as a potential scaffold for development of VEGFR-2, ERK-2 and Abl-1 multikinase inhibitor.

Jin F, Gao D, Wu Q, Liu F, Chen Y, Tan C, Jiang Y.

Bioorg Med Chem. 2013 Sep 15;21(18):5694-706. doi: 10.1016/j.bmc.2013.07.026. Epub 2013 Jul 20.

PMID:
23932071
17.

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
18.

Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors.

Wang B, Deng Y, Chen Y, Yu K, Wang A, Liang Q, Wang W, Chen C, Wu H, Hu C, Miao W, Hur W, Wang W, Hu Z, Weisberg EL, Wang J, Ren T, Wang Y, Gray NS, Liu Q, Liu J.

Eur J Med Chem. 2017 Sep 8;137:545-557. doi: 10.1016/j.ejmech.2017.06.016. Epub 2017 Jun 9.

PMID:
28628824
19.

Ethyl 2-(benzylidene)-7-methyl-3-oxo-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-6-carboxylate analogues as a new scaffold for protein kinase casein kinase 2 inhibitor.

Jin CH, Jun KY, Lee E, Kim S, Kwon Y, Kim K, Na Y.

Bioorg Med Chem. 2014 Sep 1;22(17):4553-65. doi: 10.1016/j.bmc.2014.07.037. Epub 2014 Jul 30.

PMID:
25131958
20.

2,4-Diarylamino-pyrimidines as kinase inhibitors co-targeting IGF1R and EGFR(L⁸⁵⁸R/T⁷⁹⁰M).

Chan S, Han K, Qu R, Tong L, Li Y, Zhang Z, Cheng H, Lu X, Patterson A, Smaill J, Ren X, Ding J, Xie H, Ding K.

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4277-81. doi: 10.1016/j.bmcl.2015.07.089. Epub 2015 Jul 30.

PMID:
26259806

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