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J Med Chem. 2007 Nov 1;50(22):5253-6. Epub 2007 Sep 21.

Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.

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Department of Medicinal Chemistry, Pfizer Global Research and Development, La Jolla, Inc., 10770 Science Center Drive, San Diego, California 92121-1194, USA.


The cocrystal structure of a library hit was used to design a novel series of CHK1 inhibitors. The new series retained the critical hydrogen-bonding groups of the resorcinol moiety for binding but lacked the phenolic anilide moiety. The newly designed compounds exhibited similar enzymatic activity, while demonstrating increased cellular potency. Compound 10c, showing no single agent effect, potentiated the antiproliferative effect of Gemcitabine in both prostate and breast cancer cell lines.

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