Phthalazinone-based lactams and cyclic ureas as ROCK2 selective inhibitors.

Hu, Zilun; Sitkoff, Doree; Glunz, Peter W; Zou, Yan; Wang, Cailan; Muckelbauer, Jodi K; Adam, Leonard P; Wexler, Ruth R; Quan, Mimi L

Hu, Zilun; Sitkoff, Doree; Glunz, Peter W; Zou, Yan; Wang, Cailan; Muckelbauer, Jodi K; Adam, Leonard P; Wexler, Ruth R; Quan, Mimi L.

Afiliación

Hu Z; Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA. Electronic address: zilun.hu@bms.com.
Sitkoff D; Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA.
Glunz PW; Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA.
Zou Y; Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA.
Wang C; Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA.
Muckelbauer JK; Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA.
Adam LP; Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA.
Wexler RR; Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA.
Quan ML; Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA.

Bioorg Med Chem Lett ; 88: 129304, 2023 05 15.

Article en En | MEDLINE | ID: mdl-37119973

ABSTRACT

ABSTRACT

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.

Asunto(s)

Amidas; Lactamas; Quinasas Asociadas a rho; Lactamas/farmacología; Isoformas de Proteínas; Quinasas Asociadas a rho/antagonistas & inhibidores

Palabras clave

Lactam; Phthalazinone; ROCK2 selective inhibitor; Rho kinase; X-ray crystal structure

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Quinasas Asociadas a rho / Amidas / Lactamas Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2023 Tipo del documento: Article

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