Structural highlights
Publication Abstract from PubMed
A novel series of CHK1 inhibitors based on thienopyridine template has been designed and synthesized. These inhibitors maintain critical hydrogen bonding with the hinge and conserved water in the ATP binding site. Several compounds show single digit nanomolar CHK1 activities. Compound 70 shows excellent enzymatic activity of 1 nM.
Design, synthesis and SAR of thienopyridines as potent CHK1 inhibitors.,Zhao L, Zhang Y, Dai C, Guzi T, Wiswell D, Seghezzi W, Parry D, Fischmann T, Siddiqui MA Bioorg Med Chem Lett. 2010 Dec 15;20(24):7216-21. Epub 2010 Oct 26. PMID:21074424[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Zhao L, Zhang Y, Dai C, Guzi T, Wiswell D, Seghezzi W, Parry D, Fischmann T, Siddiqui MA. Design, synthesis and SAR of thienopyridines as potent CHK1 inhibitors. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7216-21. Epub 2010 Oct 26. PMID:21074424 doi:10.1016/j.bmcl.2010.10.105
