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Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.

ABSTRACT: In this paper we describe a series of 3-cyano-5-aryl-7-aminopyrazolo[1,5-a]pyrimidine hits identified by kinase-focused subset screening as starting points for the structure-based design of conformationally constrained 6-acetamido-indole inhibitors of CK2. The synthesis, SAR, and effects of this novel series on Akt signaling and cell proliferation in vitro are described.

SUBMITTER: Dowling JE

PROVIDER: S-EPMC4025639 | biostudies-literature | 2012 Apr

REPOSITORIES: biostudies-literature

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Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.

Dowling James E JE Chuaqui Claudio C Pontz Timothy W TW Lyne Paul D PD Larsen Nicholas A NA Block Michael H MH Chen Huawei H Su Nancy N Wu Allan A Russell Daniel D Pollard Hannah H Lee John W JW Peng Bo B Thakur Kumar K Ye Qing Q Zhang Tao T Brassil Patrick P Racicot Vicki V Bao Larry L Denz Christopher R CR Cooke Emma E

ACS medicinal chemistry letters 20120124 4

In this paper we describe a series of 3-cyano-5-aryl-7-aminopyrazolo[1,5-a]pyrimidine hits identified by kinase-focused subset screening as starting points for the structure-based design of conformationally constrained 6-acetamido-indole inhibitors of CK2. The synthesis, SAR, and effects of this novel series on Akt signaling and cell proliferation in vitro are described. ...[more]

PMID: 24900464

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