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ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.

Gao H, Marhefka C, Jacobs MD, Cao J, Bandarage UK, Green J
Bioorg Med Chem Lett 28 2616-2621 (2018)
Cited: 1 times
EuropePMC logo PMID: 29945794

Abstract

Solubilizing groups have been frequently appended to kinase inhibitor drug molecules when solubility is insufficient for pharmaceutical development. Such groups are usually located at substitution sites that have minimal impact on target activity. In this report we describe the incorporation of solubilizing groups in a class of Rho kinase (ROCK) inhibitors that not only confer improved solubility, but also enhance target potency and selectivity against a closely related kinase, PKA.

Articles citing this publication (1)

  1. Design and Synthesis of New 4-(3,4,5-Trimethoxyphenyl)Thiazole-Pyrimidine Derivatives as Potential Antiproliferative Agents. El-Damasy AK, Jin H, Sabry MA, Kim HJ, Alanazi MM, Seo SH, Bang EK, Keum G. Medicina (Kaunas) 59 1076 (2023)


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