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McCoull W, Hennessy EJ, Blades K, et al. Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. ACS Med Chem Lett. 2016;7(12):1118-1123doi: 10.1021/acsmedchemlett.6b00322.
McCoull, W., Hennessy, E. J., Blades, K., Chuaqui, C., Dowling, J. E., Ferguson, A. D., Goldberg, F. W., Howe, N., Jones, C. R., Kemmitt, P. D., Lamont, G., Varnes, J. G., Ward, R. A., & Yang, B. (2016). Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. ACS medicinal chemistry letters, 7(12), 1118-1123. https://doi.org/10.1021/acsmedchemlett.6b00322
McCoull, William, et al. "Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors." ACS medicinal chemistry letters vol. 7,12 (2016): 1118-1123. doi: https://doi.org/10.1021/acsmedchemlett.6b00322
McCoull W, Hennessy EJ, Blades K, Chuaqui C, Dowling JE, Ferguson AD, Goldberg FW, Howe N, Jones CR, Kemmitt PD, Lamont G, Varnes JG, Ward RA, Yang B. Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. ACS Med Chem Lett. 2016 Sep 14;7(12):1118-1123. doi: 10.1021/acsmedchemlett.6b00322. eCollection 2016 Dec 08. PMID: 27994749; PMCID: PMC5150691.
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ACS Med Chem Lett. 2016 Sep 14;7(12):1118-1123. doi: 10.1021/acsmedchemlett.6b00322. eCollection 2016 Dec 08.

Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors.

ACS medicinal chemistry letters

William McCoull, Edward J Hennessy, Kevin Blades, Claudio Chuaqui, James E Dowling, Andrew D Ferguson, Frederick W Goldberg, Nicholas Howe, Christopher R Jones, Paul D Kemmitt, Gillian Lamont, Jeffrey G Varnes, Richard A Ward, Bin Yang

Affiliations

  1. AstraZeneca , 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K.
  2. AstraZeneca , Gatehouse Park, Waltham, Massachusetts 02451, United States.
  3. AstraZeneca , Alderley Park, Macclesfield, Cheshire, SK10 4TG, U.K.

PMID: 27994749 PMCID: PMC5150691 DOI: 10.1021/acsmedchemlett.6b00322

Abstract

Group I p21-activated kinase (PAK) inhibitors are indicated as important in cancer progression, but achieving high kinase selectivity has been challenging. A bis-anilino pyrimidine PAK1 inhibitor was identified and optimized through structure-based drug design to improve PAK1 potency and achieve high kinase selectivity, giving

Keywords: LLE; PAK; bis-anilino pyrimidine; kinase selectivity; probe

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