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Items: 1 to 20 of 165

1.

Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.

Li X, Zuo Y, Tang G, Wang Y, Zhou Y, Wang X, Guo T, Xia M, Ding N, Pan Z.

J Med Chem. 2014 Jun 26;57(12):5112-28. doi: 10.1021/jm4017762. Epub 2014 Jun 10.

PMID:
24915291
2.

Irreversible dual inhibitory mode: the novel Btk inhibitor PLS-123 demonstrates promising anti-tumor activity in human B-cell lymphoma.

Ding N, Li X, Shi Y, Ping L, Wu L, Fu K, Feng L, Zheng X, Song Y, Pan Z, Zhu J.

Oncotarget. 2015 Jun 20;6(17):15122-36.

3.

Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor.

Smaill JB, Palmer BD, Rewcastle GW, Denny WA, McNamara DJ, Dobrusin EM, Bridges AJ, Zhou H, Showalter HD, Winters RT, Leopold WR, Fry DW, Nelson JM, Slintak V, Elliot WL, Roberts BJ, Vincent PW, Patmore SJ.

J Med Chem. 1999 May 20;42(10):1803-15.

PMID:
10346932
4.

A novel 2,5-diaminopyrimidine-based affinity probe for Bruton's tyrosine kinase.

Zuo Y, Shi Y, Li X, Teng Y, Pan Z.

Sci Rep. 2015 Nov 4;5:16136. doi: 10.1038/srep16136.

5.

The mTOR kinase inhibitor everolimus synergistically enhances the anti-tumor effect of the Bruton's tyrosine kinase (BTK) inhibitor PLS-123 on Mantle cell lymphoma.

Li J, Wang X, Xie Y, Ying Z, Liu W, Ping L, Zhang C, Pan Z, Ding N, Song Y, Zhu J.

Int J Cancer. 2018 Jan 1;142(1):202-213. doi: 10.1002/ijc.31044. Epub 2017 Oct 16.

PMID:
28905990
6.

Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.

Smaill JB, Rewcastle GW, Loo JA, Greis KD, Chan OH, Reyner EL, Lipka E, Showalter HD, Vincent PW, Elliott WL, Denny WA.

J Med Chem. 2000 Apr 6;43(7):1380-97.

PMID:
10753475
7.

Ibrutinib: a first in class covalent inhibitor of Bruton's tyrosine kinase.

Davids MS, Brown JR.

Future Oncol. 2014 May;10(6):957-67. doi: 10.2217/fon.14.51. Review.

8.

Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.

Ge Y, Yang H, Wang C, Meng Q, Li L, Sun H, Zhen Y, Liu K, Li Y, Ma X.

Bioorg Med Chem. 2017 Jan 15;25(2):765-772. doi: 10.1016/j.bmc.2016.11.054. Epub 2016 Nov 29.

PMID:
27956037
9.

Single cell imaging of Bruton's tyrosine kinase using an irreversible inhibitor.

Turetsky A, Kim E, Kohler RH, Miller MA, Weissleder R.

Sci Rep. 2014 Apr 24;4:4782. doi: 10.1038/srep04782.

10.

Activity of the novel BCR kinase inhibitor IQS019 in preclinical models of B-cell non-Hodgkin lymphoma.

Balsas P, Esteve-Arenys A, Roldán J, Jiménez L, Rodríguez V, Valero JG, Chamorro-Jorganes A, de la Bellacasa RP, Teixidó J, Matas-Céspedes A, Moros A, Martínez A, Campo E, Sáez-Borderías A, Borrell JI, Pérez-Galán P, Colomer D, Roué G.

J Hematol Oncol. 2017 Mar 31;10(1):80. doi: 10.1186/s13045-017-0447-6.

11.

Bruton Kinase Inhibitors in Chronic Lymphocytic Leukemia.

Gozzetti A, Candi V, Brambilla CZ, Papini G, Fabbri A, Bocchia M.

Anticancer Agents Med Chem. 2017;17(8):1040-1045. doi: 10.2174/1871520616666160928153342. Review.

PMID:
27697038
12.

PI3Kδ inhibitor idelalisib in combination with BTK inhibitor ONO/GS-4059 in diffuse large B cell lymphoma with acquired resistance to PI3Kδ and BTK inhibitors.

Yahiaoui A, Meadows SA, Sorensen RA, Cui ZH, Keegan KS, Brockett R, Chen G, Quéva C, Li L, Tannheimer SL.

PLoS One. 2017 Feb 8;12(2):e0171221. doi: 10.1371/journal.pone.0171221. eCollection 2017.

13.

Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis.

Huang Z, Zhang Q, Yan L, Zhong G, Zhang L, Tan X, Wang Y.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):1954-7. doi: 10.1016/j.bmcl.2016.03.011. Epub 2016 Mar 4.

PMID:
26976214
14.

Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.

Cha MY, Lee KO, Kang SJ, Jung YH, Song JY, Choi KJ, Byun JY, Lee HJ, Lee GS, Park SB, Kim MS.

J Med Chem. 2012 Mar 22;55(6):2846-57. doi: 10.1021/jm201758g. Epub 2012 Mar 9.

PMID:
22372864
15.

Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.

Zhang CH, Zheng MW, Li YP, Lin XD, Huang M, Zhong L, Li GB, Zhang RJ, Lin WT, Jiao Y, Wu XA, Yang J, Xiang R, Chen LJ, Zhao YL, Cheng W, Wei YQ, Yang SY.

J Med Chem. 2015 May 14;58(9):3957-74. doi: 10.1021/acs.jmedchem.5b00270. Epub 2015 Apr 16.

PMID:
25835317
16.

Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor.

Liang Q, Chen Y, Yu K, Chen C, Zhang S, Wang A, Wang W, Wu H, Liu X, Wang B, Wang L, Hu Z, Wang W, Ren T, Zhang S, Liu Q, Yun CH, Liu J.

Eur J Med Chem. 2017 May 5;131:107-125. doi: 10.1016/j.ejmech.2017.03.001. Epub 2017 Mar 2.

PMID:
28315597
17.

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
18.

Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.

Ge Y, Wang C, Song S, Huang J, Liu Z, Li Y, Meng Q, Zhang J, Yao J, Liu K, Ma X, Sun X.

Eur J Med Chem. 2018 Jan 1;143:1847-1857. doi: 10.1016/j.ejmech.2017.10.080. Epub 2017 Nov 14.

PMID:
29146136
19.

Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Bruton's tyrosine kinase inhibitors.

Zou Y, Xiao J, Tu Z, Zhang Y, Yao K, Luo M, Ding K, Zhang Y, Lai Y.

Bioorg Med Chem Lett. 2016 Jul 1;26(13):3052-3059. doi: 10.1016/j.bmcl.2016.05.014. Epub 2016 May 7.

PMID:
27210433
20.

Design and synthesis of novel 2-phenylaminopyrimidine (PAP) derivatives and their antiproliferative effects in human chronic myeloid leukemia cells.

Chang S, Yin SL, Wang J, Jing YK, Dong JH.

Molecules. 2009 Oct 19;14(10):4166-79. doi: 10.3390/molecules14104166.

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