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Items: 1 to 20 of 257

1.

Potent and selective pyrazolo[1,5-a]pyrimidine based inhibitors of B-Raf(V600E) kinase with favorable physicochemical and pharmacokinetic properties.

Ren L, Laird ER, Buckmelter AJ, Dinkel V, Gloor SL, Grina J, Newhouse B, Rasor K, Hastings G, Gradl SN, Rudolph J.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1165-8. doi: 10.1016/j.bmcl.2011.11.092. Epub 2011 Nov 30.

PMID:
22196124
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.

Discovery of highly potent and selective type I B-Raf kinase inhibitors.

Wang X, Berger DM, Salaski EJ, Torres N, Hu Y, Levin JI, Powell D, Wojciechowicz D, Collins K, Frommer E.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6571-4. doi: 10.1016/j.bmcl.2009.10.030. Epub 2009 Oct 13.

PMID:
19854649
4.

Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.

Gopalsamy A, Ciszewski G, Shi M, Berger D, Hu Y, Lee F, Feldberg L, Frommer E, Kim S, Collins K, Wojciechowicz D, Mallon R.

Bioorg Med Chem Lett. 2009 Dec 15;19(24):6890-2. doi: 10.1016/j.bmcl.2009.10.074. Epub 2009 Oct 22.

PMID:
19884006
5.

Non-oxime pyrazole based inhibitors of B-Raf kinase.

Newhouse BJ, Hansen JD, Grina J, Welch M, Topalov G, Littman N, Callejo M, Martinson M, Galbraith S, Laird ER, Brandhuber BJ, Vigers G, Morales T, Woessner R, Randolph N, Lyssikatos J, Olivero A.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3488-92. doi: 10.1016/j.bmcl.2010.12.038. Epub 2010 Dec 17.

PMID:
21536432
6.

Pyrazolopyridine inhibitors of B-RafV600E. Part 2: structure-activity relationships.

Wenglowsky S, Ahrendt KA, Buckmelter AJ, Feng B, Gloor SL, Gradl S, Grina J, Hansen JD, Laird ER, Lunghofer P, Mathieu S, Moreno D, Newhouse B, Ren L, Risom T, Rudolph J, Seo J, Sturgis HL, Voegtli WC, Wen Z.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5533-7. doi: 10.1016/j.bmcl.2011.06.097. Epub 2011 Jul 2.

PMID:
21802293
7.

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
8.

3-Amino-pyrazolo[3,4-d]pyrimidines as p38α kinase inhibitors: design and development to a highly selective lead.

Soth M, Abbot S, Abubakari A, Arora N, Arzeno H, Billedeau R, Dewdney N, Durkin K, Frauchiger S, Ghate M, Goldstein DM, Hill RJ, Kuglstatter A, Li F, Loe B, McCaleb K, McIntosh J, Papp E, Park J, Stahl M, Sung ML, Suttman R, Swinney DC, Weller P, Wong B, Zecic H, Gabriel T.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3452-6. doi: 10.1016/j.bmcl.2011.03.098. Epub 2011 Apr 1.

PMID:
21515047
9.

The discovery of potent and selective pyridopyrimidin-7-one based inhibitors of B-RafV600E kinase.

Ren L, Ahrendt KA, Grina J, Laird ER, Buckmelter AJ, Hansen JD, Newhouse B, Moreno D, Wenglowsky S, Dinkel V, Gloor SL, Hastings G, Rana S, Rasor K, Risom T, Sturgis HL, Voegtli WC, Mathieu S.

Bioorg Med Chem Lett. 2012 May 15;22(10):3387-91. doi: 10.1016/j.bmcl.2012.04.015. Epub 2012 Apr 10.

PMID:
22534450
10.

Pyrazolopyridine inhibitors of B-Raf(V600E). Part 4: rational design and kinase selectivity profile of cell potent type II inhibitors.

Wenglowsky S, Moreno D, Laird ER, Gloor SL, Ren L, Risom T, Rudolph J, Sturgis HL, Voegtli WC.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6237-41. doi: 10.1016/j.bmcl.2012.08.007. Epub 2012 Aug 10.

PMID:
22954737
11.

B-Raf kinase inhibitors: hit enrichment through scaffold hopping.

Gopalsamy A, Shi M, Hu Y, Lee F, Feldberg L, Frommer E, Kim S, Collins K, Wojciechowicz D, Mallon R.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2431-4. doi: 10.1016/j.bmcl.2010.03.030. Epub 2010 Mar 9.

PMID:
20307980
12.

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
13.

Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.

Gopalsamy A, Ciszewski G, Hu Y, Lee F, Feldberg L, Frommer E, Kim S, Collins K, Wojciechowicz D, Mallon R.

Bioorg Med Chem Lett. 2009 May 15;19(10):2735-8. doi: 10.1016/j.bmcl.2009.03.129. Epub 2009 Mar 28.

PMID:
19362830
14.

Potent and selective pyrazole-based inhibitors of B-Raf kinase.

Hansen JD, Grina J, Newhouse B, Welch M, Topalov G, Littman N, Callejo M, Gloor S, Martinson M, Laird E, Brandhuber BJ, Vigers G, Morales T, Woessner R, Randolph N, Lyssikatos J, Olivero A.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4692-5. doi: 10.1016/j.bmcl.2008.07.002. Epub 2008 Jul 5.

PMID:
18676143
15.

Discovery and optimization of pyrazoline compounds as B-Raf inhibitors.

Duffey MO, Adams R, Blackburn C, Chau RW, Chen S, Galvin KM, Garcia K, Gould AE, Greenspan PD, Harrison S, Huang SC, Kim MS, Kulkarni B, Langston S, Liu JX, Ma LT, Menon S, Nagayoshi M, Rowland RS, Vos TJ, Xu T, Yang JJ, Yu S, Zhang Q.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4800-4. doi: 10.1016/j.bmcl.2010.06.113. Epub 2010 Jun 25.

PMID:
20634068
16.

Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase.

Wenglowsky S, Ren L, Grina J, Hansen JD, Laird ER, Moreno D, Dinkel V, Gloor SL, Hastings G, Rana S, Rasor K, Sturgis HL, Voegtli WC, Vigers G, Willis B, Mathieu S, Rudolph J.

Bioorg Med Chem Lett. 2014 Apr 15;24(8):1923-7. doi: 10.1016/j.bmcl.2014.03.007. Epub 2014 Mar 13.

PMID:
24675381
17.

Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.

Kopecky DJ, Hao X, Chen Y, Fu J, Jiao X, Jaen JC, Cardozo MG, Liu J, Wang Z, Walker NP, Wesche H, Li S, Farrelly E, Xiao SH, Kayser F.

Bioorg Med Chem Lett. 2008 Dec 15;18(24):6352-6. doi: 10.1016/j.bmcl.2008.10.092. Epub 2008 Nov 1.

PMID:
18993068
18.

Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.

Mathieu S, Gradl SN, Ren L, Wen Z, Aliagas I, Gunzner-Toste J, Lee W, Pulk R, Zhao G, Alicke B, Boggs JW, Buckmelter AJ, Choo EF, Dinkel V, Gloor SL, Gould SE, Hansen JD, Hastings G, Hatzivassiliou G, Laird ER, Moreno D, Ran Y, Voegtli WC, Wenglowsky S, Grina J, Rudolph J.

J Med Chem. 2012 Mar 22;55(6):2869-81. doi: 10.1021/jm300016v. Epub 2012 Feb 29.

PMID:
22335519
19.

Novel pyrazolopyrimidines as highly potent B-Raf inhibitors.

Di Grandi MJ, Berger DM, Hopper DW, Zhang C, Dutia M, Dunnick AL, Torres N, Levin JI, Diamantidis G, Zapf CW, Bloom JD, Hu Y, Powell D, Wojciechowicz D, Collins K, Frommer E.

Bioorg Med Chem Lett. 2009 Dec 15;19(24):6957-61. doi: 10.1016/j.bmcl.2009.10.058. Epub 2009 Oct 28.

PMID:
19875283
20.

Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors.

Blackburn C, Duffey MO, Gould AE, Kulkarni B, Liu JX, Menon S, Nagayoshi M, Vos TJ, Williams J.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4795-9. doi: 10.1016/j.bmcl.2010.06.110. Epub 2010 Jun 25.

PMID:
20630752

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