Download MendeleyDesign, 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, M.A.(2010) Bioorg Med Chem Lett 20: 7216-7221
- PubMed: 21074424
- DOI: https://doi.org/10.1016/j.bmcl.2010.10.105
- Primary Citation of Related Structures:
3PA3, 3PA4, 3PA5 - PubMed Abstract:
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.
Organizational Affiliation:
Department of Chemistry, Merck Research Laboratories, Cambridge, MA 02141, USA. [email protected]
