期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 33, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127749
关键词
TNIK inhibitor; 1H-pyrrolo[2,3-b]pyridine; IL-2 secretion inhibitory
资金
- Personalized Medicines-Molecular Signature-based Drug Discovery and Development, Strategic Priority Research Program of the Chinese Academy of Sciences [XDA12020377]
- National Science & Technology Major Project Key New Drug Creation and Manufacturing Program of China [2018ZX09711002-004]
In an in-house screening, it was discovered that the 1H-pyrrolo[2,3-b]pyridine scaffold has high inhibition on TNIK. Several designed compounds showed potent TNIK inhibition with IC50 values lower than 1 nM, and some exhibited concentration-dependent characteristics of IL-2 inhibition. These results suggest new applications and prospects for TNIK inhibitors as a drug target.
In an in-house screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were designed and synthesized, among which some compounds had potent TNIK inhibition with IC50 values lower than 1 nM. Some compounds showed concentration-dependent characteristics of IL-2 inhibition. These results provided new applications of TNIK inhibitors and new prospects of TNIK as a drug target.
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