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Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton's Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis.

Kawahata W, Asami T, Kiyoi T, Irie T, Taniguchi H, Asamitsu Y, Inoue T, Miyake T, Sawa M
J Med Chem 61 8917-8933 (2018)
Cited: 5 times
EuropePMC logo PMID: 30216722

Abstract

Bruton's tyrosine kinase (BTK) is a promising drug target for the treatment of multiple diseases, such as B-cell malignances, asthma, and rheumatoid arthritis. A series of novel aminotriazines were identified as highly selective inhibitors of BTK by a scaffold-hopping approach. Subsequent SAR studies of this series using two conformationally different BTK proteins, an activated form of BTK and an unactivated form of BTK, led to the discovery of a highly selective BTK inhibitor, 4b. With significant efficacy in models in vivo and good ADME and safety profiles, 4b was advanced into preclinical studies.

Reviews citing this publication (3)

  1. Recent Advances in BTK Inhibitors for the Treatment of Inflammatory and Autoimmune Diseases. Zhang D, Gong H, Meng F. Molecules 26 4907 (2021)
  2. The Development of BTK Inhibitors: A Five-Year Update. Tasso B, Spallarossa A, Russo E, Brullo C. Molecules 26 7411 (2021)
  3. Harnessing the cyclization strategy for new drug discovery. Tang K, Wang S, Gao W, Song Y, Yu B. Acta Pharm Sin B 12 4309-4326 (2022)

Articles citing this publication (2)

  1. Accelerating Drug Discovery by Early Protein Drug Target Prediction Based on a Multi-Fingerprint Similarity Search. Montaruli M, Alberga D, Ciriaco F, Trisciuzzi D, Tondo AR, Mangiatordi GF, Nicolotti O. Molecules 24 E2233 (2019)
  2. Boosting the predictive performance with aqueous solubility dataset curation. Meng J, Chen P, Wahib M, Yang M, Zheng L, Wei Y, Feng S, Liu W. Sci Data 9 71 (2022)


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