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Start Over Author "Kim, Jihyung" Journal bulletin of the korean chemical society
2 results on '"Kim, Jihyung"'

2. Discovery of novel thienopyrimidine derivatives as LRRK2 inhibitors.

Author

Choi, Changyu, Park, Jiwon, Jang, Soyeon, Kim, Jihyung, Lee, Sohee, and Min, Kyung Hoon

Subjects
DARDARIN, CROHN'S disease, PYRIMIDINES, PARKINSON'S disease, STRUCTURE-activity relationships
Abstract

Leucine‐rich repeat kinase 2 (LRRK2) is considered a promising therapeutic target for Parkinson's disease, Crohn's disease, and cancer. Despite considerable research, none of these inhibitors are available for clinical application. Herein, we designed and synthesized novel thienopyrimidine derivatives by a bioisosteric replacement and investigated their structure–activity relationships. Thieno[3,2‐d]pyrimidine derivative 22 showed the most potent inhibitory activity and inhibited both wild‐type and G2019S mutant LRRK2 with IC50 values of 30 and 14 nM, respectively. [ABSTRACT FROM AUTHOR]

Published
2022
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