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Items: 1 to 20 of 130

1.

Synthesis, biological evaluation and molecular docking of novel 5-phenyl-1H-pyrazol derivatives as potential BRAF(V600E) inhibitors.

Dong JJ, Li QS, Wang SF, Li CY, Zhao X, Qiu HY, Zhao MY, Zhu HL.

Org Biomol Chem. 2013 Oct 7;11(37):6328-37. doi: 10.1039/c3ob40776d.

PMID:
23942809
2.

Design, synthesis and biological evaluation of novel 5-phenyl-1H-pyrazole derivatives as potential BRAF(V600E) inhibitors.

Wang SF, Zhu YL, Zhu PT, Makawana JA, Zhang YL, Zhao MY, Lv PC, Zhu HL.

Bioorg Med Chem. 2014 Nov 1;22(21):6201-8. doi: 10.1016/j.bmc.2014.08.029. Epub 2014 Sep 6.

PMID:
25267006
3.

Synthesis, biological evaluation of novel 4,5-dihydro-2H-pyrazole 2-hydroxyphenyl derivatives as BRAF inhibitors.

Liu JJ, Zhang H, Sun J, Wang ZC, Yang YS, Li DD, Zhang F, Gong HB, Zhu HL.

Bioorg Med Chem. 2012 Oct 15;20(20):6089-96. doi: 10.1016/j.bmc.2012.08.020. Epub 2012 Aug 25.

PMID:
22985957
4.

Synthesis, biological evaluation and 3D-QSAR study of novel 4,5-dihydro-1H-pyrazole thiazole derivatives as BRAF(V⁶⁰⁰E) inhibitors.

Zhao MY, Yin Y, Yu XW, Sangani CB, Wang SF, Lu AM, Yang LF, Lv PC, Jiang MG, Zhu HL.

Bioorg Med Chem. 2015 Jan 1;23(1):46-54. doi: 10.1016/j.bmc.2014.11.029. Epub 2014 Nov 26.

PMID:
25496804
5.

Synthesis, biological evaluation and 3D-QSAR studies of novel 4,5-dihydro-1H-pyrazole niacinamide derivatives as BRAF inhibitors.

Li CY, Li QS, Yan L, Sun XG, Wei R, Gong HB, Zhu HL.

Bioorg Med Chem. 2012 Jun 15;20(12):3746-55. doi: 10.1016/j.bmc.2012.04.047. Epub 2012 Apr 28.

PMID:
22583669
6.

Identification of novel 3,5-diarylpyrazoline derivatives containing salicylamide moiety as potential anti-melanoma agents.

Li QS, Lv XH, Zhang YB, Dong JJ, Zhou WP, Yang Y, Zhu HL.

Bioorg Med Chem Lett. 2012 Nov 1;22(21):6596-601. doi: 10.1016/j.bmcl.2012.09.004. Epub 2012 Sep 10.

PMID:
23025996
7.

Design, modification and 3D QSAR studies of novel 2,3-dihydrobenzo[b][1,4]dioxin-containing 4,5-dihydro-1H-pyrazole derivatives as inhibitors of B-Raf kinase.

Yang YS, Li QS, Sun S, Zhang YB, Wang XL, Zhang F, Tang JF, Zhu HL.

Bioorg Med Chem. 2012 Oct 15;20(20):6048-58. doi: 10.1016/j.bmc.2012.08.043. Epub 2012 Aug 30.

PMID:
22985962
8.

Modification, biological evaluation and 3D QSAR studies of novel 2-(1,3-diaryl- 4,5-dihydro-1H-pyrazol-5-yl)phenol derivatives as inhibitors of B-Raf kinase.

Yang YS, Zhang F, Tang DJ, Yang YH, Zhu HL.

PLoS One. 2014 May 14;9(5):e95702. doi: 10.1371/journal.pone.0095702. eCollection 2014.

9.

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
10.

Discovery and pharmacophore studies of novel pyrazole-based anti-melanoma agents.

Li QS, Lü XH, Yang Y, Ruan BF, Yao RS, Liao CZ.

Chem Biodivers. 2015 Jan;12(1):116-32. doi: 10.1002/cbdv.201400143.

PMID:
25641840
11.

Design, synthesis and evaluation of novel 2-(1H-imidazol-2-yl) pyridine Sorafenib derivatives as potential BRAF inhibitors and anti-tumor agents.

Jiao Y, Xin BT, Zhang Y, Wu J, Lu X, Zheng Y, Tang W, Zhou X.

Eur J Med Chem. 2015 Jan 27;90:170-83. doi: 10.1016/j.ejmech.2014.11.008. Epub 2014 Nov 6.

PMID:
25461318
12.

Design, synthesis and biological evaluation of novel (E)-α-benzylsulfonyl chalcone derivatives as potential BRAF inhibitors.

Li QS, Li CY, Lu X, Zhang H, Zhu HL.

Eur J Med Chem. 2012 Apr;50:288-95. doi: 10.1016/j.ejmech.2012.02.007. Epub 2012 Feb 11.

PMID:
22361686
13.

Synthesis, biological evaluation, and molecular docking studies of N-((1,3-diphenyl-1H-pyrazol-4-yl)methyl)aniline derivatives as novel anticancer agents.

Huang XF, Lu X, Zhang Y, Song GQ, He QL, Li QS, Yang XH, Wei Y, Zhu HL.

Bioorg Med Chem. 2012 Aug 15;20(16):4895-900. doi: 10.1016/j.bmc.2012.06.056. Epub 2012 Jul 10.

PMID:
22819191
14.

New diarylureas and diarylamides containing 1,3,4-triarylpyrazole scaffold: Synthesis, antiproliferative evaluation against melanoma cell lines, ERK kinase inhibition, and molecular docking studies.

Choi WK, El-Gamal MI, Choi HS, Baek D, Oh CH.

Eur J Med Chem. 2011 Dec;46(12):5754-62. doi: 10.1016/j.ejmech.2011.08.013. Epub 2011 Aug 12.

PMID:
22014559
16.

Design, biological evaluation and 3D QSAR studies of novel dioxin-containing triaryl pyrazoline derivatives as potential B-Raf inhibitors.

Yang YS, Yang B, Zou Y, Li G, Zhu HL.

Bioorg Med Chem. 2016 Jul 1;24(13):3052-3061. doi: 10.1016/j.bmc.2016.05.012. Epub 2016 May 12.

PMID:
27238841
17.

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
18.

Design, synthesis and biological evaluation of benzyl 2-(1H-imidazole-1-yl) pyrimidine analogues as selective and potent Raf inhibitors.

Kim M, Lee J, Jung K, Kim H, Aman W, Ryu JS, Hah JM.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3600-4. doi: 10.1016/j.bmcl.2014.05.030. Epub 2014 May 17.

PMID:
24878193
19.

Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.

Henry JR, Kaufman MD, Peng SB, Ahn YM, Caldwell TM, Vogeti L, Telikepalli H, Lu WP, Hood MM, Rutkoski TJ, Smith BD, Vogeti S, Miller D, Wise SC, Chun L, Zhang X, Zhang Y, Kays L, Hipskind PA, Wrobleski AD, Lobb KL, Clay JM, Cohen JD, Walgren JL, McCann D, Patel P, Clawson DK, Guo S, Manglicmot D, Groshong C, Logan C, Starling JJ, Flynn DL.

J Med Chem. 2015 May 28;58(10):4165-79. doi: 10.1021/acs.jmedchem.5b00067. Epub 2015 May 12.

PMID:
25965804
20.

CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity.

James J, Ruggeri B, Armstrong RC, Rowbottom MW, Jones-Bolin S, Gunawardane RN, Dobrzanski P, Gardner MF, Zhao H, Cramer MD, Hunter K, Nepomuceno RR, Cheng M, Gitnick D, Yazdanian M, Insko DE, Ator MA, Apuy JL, Faraoni R, Dorsey BD, Williams M, Bhagwat SS, Holladay MW.

Mol Cancer Ther. 2012 Apr;11(4):930-41. doi: 10.1158/1535-7163.MCT-11-0645. Epub 2012 Feb 7.

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