Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors

[Display omitted] 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 concentra...

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Published inBioorganic & medicinal chemistry letters Vol. 33; p. 127749
Main Authors Yang, Bowen, Wu, Qian, Huan, Xiajuan, Wang, Yingqing, Sun, Yin, Yang, Yueyue, Liu, Tongchao, Wang, Xin, Chen, Lin, Xiong, Bing, Zhao, Dongmei, Miao, Zehong, Chen, Danqi
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 01.02.2021
Elsevier
Subjects
1H-pyrrolo[2,3-b]pyridine
Chemistry
Chemistry, Medicinal
Chemistry, Organic
IL-2 secretion inhibitory
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
TNIK inhibitor
TNIK inhibitor
1H-pyrrolo[2,3-b]pyridine
IL-2 secretion inhibitory
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Summary:[Display omitted] 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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ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2020.127749