Publication details

Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 1.

Authors

DWYER Michael PARUCH Kamil LABROLI Marc ALVAREZ Carmen KEERTIKAR Kerry POKER Cory ROSSMAN Randall FISCHMANN Thierry DUCA Jose MADISON Vincent PARRY David DAVIS Nicole SEGHEZZI Wolfgang WISWELL Derek GUZI Timothy

Year of publication 2011
Type Article in Periodical
Magazine / Source Bioorganic & Medicinal Chemistry Letters
MU Faculty or unit

Faculty of Science

Citation
Field Organic chemistry
Keywords Kinase CHK1 Pyrazolo[1 5-a]pyrimidine Template
Description The synthesis and hit-to-lead SAR development of a pyrazolo[1,5-a]pyrimidine hit 4 is described leading to a series of potent, selective CHK1 inhibitors such as compound 17r. In the Letter, the further utility of the pyrazolo[1,5-a]pyrimidine template for the development of potent, selective kinase inhibitors is detailed.

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