Discovery and biological evaluation of N5-substituted 6,7-dioxo-6,7-dihydropteridine derivatives as potent Bruton's tyrosine kinase inhibitors

Haiyang Chen; Peiran Song; Yanyan Diao; Yongjia Hao; Dou Dou; Wanqi Wang; Xiaoyu Fang; Yanling Wang; Zhenjiang Zhao; Jian Ding; Honglin Li; Hua Xie; Yufang Xu

doi:10.1039/c8md00019k

Discovery and biological evaluation of N5-substituted 6,7-dioxo-6,7-dihydropteridine derivatives as potent Bruton's tyrosine kinase inhibitors

MedChemComm ◽

10.1039/c8md00019k ◽

2018 ◽

Vol 9 (4) ◽

pp. 697-704 ◽

Cited By ~ 2

Author(s):

Haiyang Chen ◽

Peiran Song ◽

Yanyan Diao ◽

Yongjia Hao ◽

Dou Dou ◽

...

Keyword(s):

Tyrosine Kinase ◽

Enzymatic Activity ◽

Tyrosine Kinase Inhibitors ◽

Kinase Inhibitors ◽

Biological Evaluation ◽

Bruton’S Tyrosine Kinase ◽

Bruton's Tyrosine Kinase

Compound6potently inhibited the enzymatic activity of BTK with an IC50value of 1.9 nM.

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Discovery and biological evaluation of N-(3-(7-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-4-methyl-2-oxo-2H-pyrimido[4,5-d][1,3]oxazin-1(4H)-yl)phenyl)acrylamide as potent Bruton’s tyrosine kinase inhibitors

Acta Pharmacologica Sinica ◽

10.1038/s41401-019-0250-8 ◽

2019 ◽

Vol 41 (3) ◽

pp. 415-422

Author(s):

Meng-zhen Lai ◽

Pei-ran Song ◽

Dou Dou ◽

Yan-yan Diao ◽

Lin-jiang Tong ◽

...

Keyword(s):

Tyrosine Kinase ◽

Tyrosine Kinase Inhibitors ◽

Kinase Inhibitors ◽

Biological Evaluation ◽

Bruton’S Tyrosine Kinase ◽

Bruton's Tyrosine Kinase

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Discovery and Biological evaluation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives as potent Bruton’s tyrosine kinase inhibitors

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2019.06.023 ◽

2019 ◽

Vol 27 (15) ◽

pp. 3390-3395 ◽

Cited By ~ 1

Author(s):

Yanyan Diao ◽

Xiaoyu Fang ◽

Peiran Song ◽

Mengzhen Lai ◽

Linjiang Tong ◽

...

Keyword(s):

Tyrosine Kinase ◽

Tyrosine Kinase Inhibitors ◽

Kinase Inhibitors ◽

Biological Evaluation ◽

Bruton’S Tyrosine Kinase ◽

Bruton's Tyrosine Kinase

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Faculty Opinions recommendation of Aminopyrazole Carboxamide Bruton’s Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.734569206.793554988 ◽

2019 ◽

Author(s):

John Lowe

Keyword(s):

Tyrosine Kinase ◽

Tyrosine Kinase Inhibitors ◽

Kinase Inhibitors ◽

Bruton’S Tyrosine Kinase ◽

Reactive Group ◽

Bruton's Tyrosine Kinase ◽

Reversible Covalent

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Bruton’s Tyrosine Kinase Inhibitors for the Treatment of Autoimmune Diseases and Cancers

ACS Medicinal Chemistry Letters ◽

10.1021/acsmedchemlett.7b00331 ◽

2017 ◽

Vol 8 (9) ◽

pp. 911-913

Author(s):

Robert B. Kargbo

Keyword(s):

Tyrosine Kinase ◽

Autoimmune Diseases ◽

Tyrosine Kinase Inhibitors ◽

Kinase Inhibitors ◽

Bruton’S Tyrosine Kinase ◽

Bruton's Tyrosine Kinase

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The safety of Bruton’s tyrosine kinase inhibitors for the treatment of chronic lymphocytic leukemia

Expert Opinion on Drug Safety ◽

10.1080/14740338.2017.1344213 ◽

2017 ◽

Vol 16 (9) ◽

pp. 1079-1088 ◽

Cited By ~ 7

Author(s):

Phu N. Tran ◽

Susan O’Brien

Keyword(s):

Chronic Lymphocytic Leukemia ◽

Tyrosine Kinase ◽

Tyrosine Kinase Inhibitors ◽

Kinase Inhibitors ◽

Lymphocytic Leukemia ◽

Bruton’S Tyrosine Kinase ◽

Bruton's Tyrosine Kinase

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A Pharmacokinetic/Pharmacodynamic Perspective on the Effect of Bruton's Tyrosine Kinase Inhibitors on Collagen-Induced Platelet Aggregation

Clinical Lymphoma Myeloma & Leukemia ◽

10.1016/j.clml.2016.07.177 ◽

2016 ◽

Vol 16 ◽

pp. S121

Author(s):

Jun Chen ◽

Taisei Kinoshita ◽

Tarikere Gururaja ◽

Juthamas Sukbuntherng ◽

Danelle James ◽

...

Keyword(s):

Platelet Aggregation ◽

Tyrosine Kinase ◽

Tyrosine Kinase Inhibitors ◽

Kinase Inhibitors ◽

Bruton’S Tyrosine Kinase ◽

Bruton's Tyrosine Kinase

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

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2016.05.014 ◽

2016 ◽

Vol 26 (13) ◽

pp. 3052-3059 ◽

Cited By ~ 4

Author(s):

Yi Zou ◽

Jianhu Xiao ◽

Zhengchao Tu ◽

Yingyi Zhang ◽

Kun Yao ◽

...

Keyword(s):

Tyrosine Kinase ◽

Tyrosine Kinase Inhibitors ◽

Kinase Inhibitors ◽

Bruton’S Tyrosine Kinase ◽

Bruton's Tyrosine Kinase

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P3612Potential for Bruton's tyrosine kinase inhibitors as additional antiplatelet agents in acute coronary syndromes

European Heart Journal ◽

10.1093/eurheartj/ehy563.p3612 ◽

2018 ◽

Vol 39 (suppl_1) ◽

Author(s):

M Bhatti ◽

O Michail ◽

S Ayton ◽

N D Gollop ◽

A Ryding ◽

...

Keyword(s):

Tyrosine Kinase ◽

Tyrosine Kinase Inhibitors ◽

Acute Coronary Syndromes ◽

Kinase Inhibitors ◽

Antiplatelet Agents ◽

Bruton’S Tyrosine Kinase ◽

Bruton's Tyrosine Kinase ◽

Coronary Syndromes

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Pharmacophore modeling and virtual screening in search of novel Bruton’s tyrosine kinase inhibitors

Journal of Molecular Modeling ◽

10.1007/s00894-019-4047-y ◽

2019 ◽

Vol 25 (7) ◽

Author(s):

Aditya Sharma ◽

B. K. Thelma

Keyword(s):

Virtual Screening ◽

Tyrosine Kinase ◽

Tyrosine Kinase Inhibitors ◽

Kinase Inhibitors ◽

Pharmacophore Modeling ◽

Bruton’S Tyrosine Kinase ◽

Bruton's Tyrosine Kinase

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Bruton's tyrosine kinase inhibitors in B-cell non-Hodgkin's lymphomas

Clinical Pharmacology & Therapeutics ◽

10.1002/cpt.65 ◽

2015 ◽

Vol 97 (5) ◽

pp. 469-477 ◽

Cited By ~ 16

Author(s):

L Alinari ◽

C Quinion ◽

KA Blum

Keyword(s):

Tyrosine Kinase ◽

B Cell ◽

Tyrosine Kinase Inhibitors ◽

Kinase Inhibitors ◽

Bruton’S Tyrosine Kinase ◽

Bruton's Tyrosine Kinase ◽

Hodgkin's Lymphomas

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