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Discovery of orally available 1H-pyrazolo [3, 4-d] pyrimidin-4-amine derivative as a novel BTK inhibitor.
- Source :
- Arabian Journal of Chemistry; Sep2024, Vol. 17 Issue 9, pN.PAG-N.PAG, 1p
- Publication Year :
- 2024
-
Abstract
- Bruton's tyrosine kinase (BTK) is a key protein in B cell antigen receptor (BCR) signaling pathway, and is a research hotspot in the clinical treatment of B cell tumors and B cell immune diseases. In this article, based on the structure of Ibrutinib, a series of novel irreversible BTK inhibitors with the scaffolding of 1H -pyrazolo [3, 4- d ] pyrimidin-4-amine were designed and synthesized. All the compounds showed a moderate to potent inhibitory activity against BTK. Among them, compound 6b showed the best BTK kinase inhibitory activity with the IC 50 value of 1.2 nM. The ADME/T properties performed by pkCSM demonstrated that compound 6b possesses a good druglikeness. Further druggability evaluation showed that 6b exhibited good water solubility and acceptable pharmacokinetic properties. Therefore, compound 6b provided a promising lead compound for developing novel irreversible BTK inhibitors. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 18785352
- Volume :
- 17
- Issue :
- 9
- Database :
- Supplemental Index
- Journal :
- Arabian Journal of Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 179106163
- Full Text :
- https://doi.org/10.1016/j.arabjc.2024.105906