5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.

@article{Vymtalov20165Substituted3W,
  title={5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.},
  author={Ladislava Vymětalov{\'a} and Libor Havl{\'i}cek and Anton{\'i}n {\vS}turc and Zuzana Skr{\'a}{\vs}kov{\'a} and Radek Jorda and Tom{\'a}{\vs} Posp{\'i}{\vs}il and Miroslav Strnad and Vladim{\'i}r Kry{\vs}tof},
  journal={European journal of medicinal chemistry},
  year={2016},
  volume={110},
  pages={291-301}
}
A series of 5-substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine derivatives was synthesized and evaluated for their cyclin-dependent kinase (CDK) inhibition activity. The most potent compounds contained various hydroxyalkylamines at the 5 position and possessed low nanomolar IC50 values for CDK2 and CDK5. Preliminary profiling of one of the most active compounds on a panel of 50 protein kinases revealed its high selectivity for CDKs. The compounds arrested… CONTINUE READING