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Items: 1 to 20 of 131

1.

4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors.

Holladay MW, Campbell BT, Rowbottom MW, Chao Q, Sprankle KG, Lai AG, Abraham S, Setti E, Faraoni R, Tran L, Armstrong RC, Gunawardane RN, Gardner MF, Cramer MD, Gitnick D, Ator MA, Dorsey BD, Ruggeri BR, Williams M, Bhagwat SS, James J.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5342-6. doi: 10.1016/j.bmcl.2011.07.019. Epub 2011 Jul 14.

PMID:
21807507
2.

Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.

Rowbottom MW, Faraoni R, Chao Q, Campbell BT, Lai AG, Setti E, Ezawa M, Sprankle KG, Abraham S, Tran L, Struss B, Gibney M, Armstrong RC, Gunawardane RN, Nepomuceno RR, Valenta I, Hua H, Gardner MF, Cramer MD, Gitnick D, Insko DE, Apuy JL, Jones-Bolin S, Ghose AK, Herbertz T, Ator MA, Dorsey BD, Ruggeri B, Williams M, Bhagwat S, James J, Holladay MW.

J Med Chem. 2012 Feb 9;55(3):1082-105. doi: 10.1021/jm2009925. Epub 2012 Jan 23.

PMID:
22168626
3.

Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents.

Lu C, Tang K, Li Y, Li P, Lin Z, Yin D, Chen X, Huang H.

Eur J Med Chem. 2014 Apr 22;77:351-60. doi: 10.1016/j.ejmech.2014.03.020. Epub 2014 Mar 12.

PMID:
24675135
4.

Design, synthesis and biological evaluation of bis-aryl ureas and amides based on 2-amino-3-purinylpyridine scaffold as DFG-out B-Raf kinase inhibitors.

Yang W, Chen Y, Zhou X, Gu Y, Qian W, Zhang F, Han W, Lu T, Tang W.

Eur J Med Chem. 2015 Jan 7;89:581-96. doi: 10.1016/j.ejmech.2014.10.039. Epub 2014 Oct 16.

PMID:
25462267
5.

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
6.

Identification of type II inhibitors targeting BRAF using privileged pharmacophores.

Zhang Q, Wang J, Wang F, Chen X, He Y, You Q, Zhou H.

Chem Biol Drug Des. 2014 Jan;83(1):27-36. doi: 10.1111/cbdd.12198. Epub 2013 Oct 25.

PMID:
24164966
7.

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
8.

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
9.

Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors.

Vasbinder MM, Aquila B, Augustin M, Chen H, Cheung T, Cook D, Drew L, Fauber BP, Glossop S, Grondine M, Hennessy E, Johannes J, Lee S, Lyne P, Mörtl M, Omer C, Palakurthi S, Pontz T, Read J, Sha L, Shen M, Steinbacher S, Wang H, Wu A, Ye M.

J Med Chem. 2013 Mar 14;56(5):1996-2015. doi: 10.1021/jm301658d. Epub 2013 Feb 27.

PMID:
23398453
10.

Structure-based de novo design and biochemical evaluation of novel BRAF kinase inhibitors.

Park H, Jeong Y, Hong S.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1027-30. doi: 10.1016/j.bmcl.2011.11.124. Epub 2011 Dec 7.

PMID:
22196123
11.

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
12.

Design and synthesis of new potent anticancer benzothiazole amides and ureas featuring pyridylamide moiety and possessing dual B-Raf(V600E) and C-Raf kinase inhibitory activities.

El-Damasy AK, Lee JH, Seo SH, Cho NC, Pae AN, Keum G.

Eur J Med Chem. 2016 Jun 10;115:201-16. doi: 10.1016/j.ejmech.2016.02.039. Epub 2016 Feb 18.

PMID:
27017549
13.

Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline.

Smith AL, DeMorin FF, Paras NA, Huang Q, Petkus JK, Doherty EM, Nixey T, Kim JL, Whittington DA, Epstein LF, Lee MR, Rose MJ, Babij C, Fernando M, Hess K, Le Q, Beltran P, Carnahan J.

J Med Chem. 2009 Oct 22;52(20):6189-92. doi: 10.1021/jm901081g.

PMID:
19764794
14.

Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors.

Cai ZW, Wei D, Schroeder GM, Cornelius LA, Kim K, Chen XT, Schmidt RJ, Williams DK, Tokarski JS, An Y, Sack JS, Manne V, Kamath A, Zhang Y, Marathe P, Hunt JT, Lombardo LJ, Fargnoli J, Borzilleri RM.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3224-9. doi: 10.1016/j.bmcl.2008.04.047. Epub 2008 Apr 25.

PMID:
18479916
15.

Synthesis of quinazolines as tyrosine kinase inhibitors.

Srivastava SK, Kumar V, Agarwal SK, Mukherjee R, Burman AC.

Anticancer Agents Med Chem. 2009 Mar;9(3):246-75. Review.

PMID:
19275520
16.

Preclinical assessment of novel BRAF inhibitors: integrating pharmacokinetic-pharmacodynamic modelling in the drug discovery process.

Choo EF, Alicke B, Boggs J, Dinkel V, Gould S, Grina J, West K, Menghrajani K, Ran Y, Rudolph J, Wenglowsky S.

Xenobiotica. 2011 Dec;41(12):1076-87. doi: 10.3109/00498254.2011.603384. Epub 2011 Aug 25.

PMID:
21864203
17.

Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors.

Ramurthy S, Subramanian S, Aikawa M, Amiri P, Costales A, Dove J, Fong S, Jansen JM, Levine B, Ma S, McBride CM, Michaelian J, Pick T, Poon DJ, Girish S, Shafer CM, Stuart D, Sung L, Renhowe PA.

J Med Chem. 2008 Nov 27;51(22):7049-52. doi: 10.1021/jm801050k.

PMID:
18942827
18.

NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.

Beria I, Bossi RT, Brasca MG, Caruso M, Ceccarelli W, Fachin G, Fasolini M, Forte B, Fiorentini F, Pesenti E, Pezzetta D, Posteri H, Scolaro A, Re Depaolini S, Valsasina B.

Bioorg Med Chem Lett. 2011 May 15;21(10):2969-74. doi: 10.1016/j.bmcl.2011.03.054. Epub 2011 Mar 21.

PMID:
21470862
19.

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
20.

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

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