Structure-activity relationships for 2-anilino-6-phenylpyrido[2,3-d]pyrimidin-7(8H)-ones as inhibitors of the cellular checkpoint kinase Wee1.

@article{Palmer2005StructureactivityRF,
  title={Structure-activity relationships for 2-anilino-6-phenylpyrido[2,3-d]pyrimidin-7(8H)-ones as inhibitors of the cellular checkpoint kinase Wee1.},
  author={Brian D. Palmer and Jeff Bruce Smaill and Gordon William Rewcastle and Ellen M Dobrusin and Alan J. Kraker and Charles W. Moore and Randall W Steinkampf and William A. Denny},
  journal={Bioorganic & medicinal chemistry letters},
  year={2005},
  volume={15 7},
  pages={1931-5}
}
A series of 2-anilino-6-phenylpyrido[2,3-d]pyrimidin-7(8H)-ones were synthesized and evaluated for their inhibitory properties against the non-receptor kinase c-Src and the G2/M checkpoint kinase Wee1. Overall, the compounds were 10-100-fold more potent inhibitors of c-Src than Wee1, and variation of substituents on the 6-phenyl ring did not markedly alter this preference. Solubilizing substituents off the 2-anilino ring in many cases increased Wee1 activity, thus lowering this preference to… CONTINUE READING