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Bioorg Med Chem Lett. 2014 Mar 15;24(6):1592-6. doi: 10.1016/j.bmcl.2014.01.058. Epub 2014 Jan 30.

2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors.

Author information

1
Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 4560 Horton Street, Emeryville, CA 94608, USA.
2
Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 4560 Horton Street, Emeryville, CA 94608, USA. Electronic address: cynthia.shafer@novartis.com.

Abstract

2-Amino-7-substituted benzoxazole analogs were identified by HTS as inhibitors of RSK2. Molecular modeling and medicinal chemistry techniques were employed to explore the SAR for this series with a focus of improving in vitro and target modulation potency and physicochemical properties.

KEYWORDS:

Benzoxazole; HTS; Heterocycle; Kinase; RSK

PMID:
24534486
DOI:
10.1016/j.bmcl.2014.01.058
[Indexed for MEDLINE]

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