Phthalazinone-based lactams and cyclic ureas as ROCK2 selective inhibitors

[Display omitted] Derivatives of lactam, cyclic urea and carbamate were explored as aniline amide replacements in a series of phthalazinone-based ROCK inhibitors. Potent ROCK2 inhibitors such as 22 were identified with excellent overall kinase selectivity as well as good isoform selectivity over ROC...

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Published inBioorganic & medicinal chemistry letters Vol. 88; pp. 129304 - 129308
Main Authors Hu, Zilun, Sitkoff, Doree, Glunz, Peter W., Zou, Yan, Wang, Cailan, Muckelbauer, Jodi K., Adam, Leonard P., Wexler, Ruth R., Quan, Mimi L.
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 15.05.2023
Elsevier
Subjects
Amides
Chemistry
Chemistry, Medicinal
Chemistry, Organic
Lactam
Lactams - pharmacology
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Phthalazinone
Physical Sciences
Protein Isoforms
Rho kinase
rho-Associated Kinases - antagonists & inhibitors
ROCK2 selective inhibitor
Science & Technology
X-ray crystal structure
Phthalazinone
X-ray crystal structure
Rho kinase
ROCK2 selective inhibitor
Lactam
RHO KINASES
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Summary:[Display omitted] Derivatives of lactam, cyclic urea and carbamate were explored as aniline amide replacements in a series of phthalazinone-based ROCK inhibitors. Potent ROCK2 inhibitors such as 22 were identified with excellent overall kinase selectivity as well as good isoform selectivity over ROCK1.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2023.129304